Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are 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:
September 6, 2005
Date of Patent:
April 13, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
Abstract: The present invention relates to methods and compositions for the treatment of pulmonary inflammation. In particular, methods and compositions using aerosol levofloxacin or ofloxacin to reduce pulmonary inflammation are provided.
Type:
Application
Filed:
October 6, 2009
Publication date:
April 8, 2010
Applicant:
MPEX PHARMACEUTICALS, INC.
Inventors:
Michael N. Dudley, Ruslan Y. Tsivkovski, David C. Griffith, Olga Rodny
Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.
Type:
Application
Filed:
October 6, 2009
Publication date:
April 8, 2010
Applicant:
MPEX PHARMACEUTICALS, INC.
Inventors:
David C. Griffith, Michael N. Dudley, Mark W. Surber, Keith A. Bostian, Olga Rodny
Abstract: The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a modified benzoxazine moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.
Abstract: The present invention relates to an improved process for the preparation of Levofloxacin hemihydrate by adjusting the moisture content of the solvent to about 12% to about 20% during crystallization.
Abstract: Disclosed herein are a collagen-based matrix for use as a restorative material and a method for the preparation thereof. An atelocollagen dispersion is spread at a predetermined thickness over a plate and freeze-dried to form a porous collagen membrane. An atelocollagen dispersion is separately spread over a plate and pressurized to form a dense collagen membrane. This is overlaid with the porous collagen membrane and immersed in an EDS solution in ethanol to crosslink the two membranes with each other. From the bilayer structure thus constructed, EDS is removed, followed by lyophilization and cutting into an appropriate size.
Type:
Application
Filed:
April 15, 2009
Publication date:
February 18, 2010
Applicant:
DALIM TISSEN Inc.
Inventors:
Seong-Ki LEE, Si-Nae Park, Sang-Hee Bae
Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.
Type:
Application
Filed:
August 28, 2009
Publication date:
January 28, 2010
Inventors:
Michael Robert Barbachyn, J. Craig Ruble, Arthur Glenn Romero, Lisa Marie Thomasco, Alexander Ross Hurd, John Raymond Palmer, Peter Laurence Toogood, Dennis Joseph McNamara, Debra Ann Sherry, Paul Joseph Dobrowolski
Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Application
Filed:
July 24, 2009
Publication date:
January 28, 2010
Applicant:
Gilead Sciences, Inc.
Inventors:
Evangelos Aktoudianakis, Azim Alan Celebi, Zhimin Du, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish, Barton W. Phillips, Joseph H. Saugier, Zheng-Yu Yang, Catalin Sebastian Zonte
Abstract: Provided are electrokinetically-altered fluids (gas-enriched (e.g., oxygen-enriched) electrokinetic fluids) comprising an ionic aqueous solution of charge-stabilized oxygen-containing nanostructures in an amount sufficient to provide, upon contact with a cell, modulation of at least one of cellular membrane potential and cellular membrane conductivity, and therapeutic compositions and methods for using same in treating cystic fibrosis or a symptom thereof. The electrokinetically-altered fluid compositions and methods include electrokinetically-altered fluids optionally in combination with other therapeutic agents (e.g., antibiotics, albuterol, budesonide, etc.). Particular embodiments comprise use and/or synergy with tobramycin for treating bacterial infection, and use and/or synergy with a bronchiodilator.
Type:
Application
Filed:
May 1, 2009
Publication date:
January 7, 2010
Applicant:
Revalesio Corporation
Inventors:
Richard L. Watson, Anthony B. Wood, Gregory J. Archambeau
Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
Type:
Application
Filed:
April 28, 2006
Publication date:
December 24, 2009
Inventors:
Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
Abstract: The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Type:
Grant
Filed:
June 27, 2005
Date of Patent:
December 15, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, Chunze Li, Lou Anne Neilson, Christy M. Olson, Edward S. Tasber
Abstract: Compounds of a certain formula (I), in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.
Type:
Application
Filed:
March 26, 2009
Publication date:
October 29, 2009
Applicant:
NYCOMED GMBH
Inventors:
Klaus PEKARI, Thomas BAER, Bjoern BARTELS, Mathias SCHMIDT, Thomas BECKERS
Abstract: The present invention is directed to quinolone derivatives, useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes
Abstract: The invention includes tetrahydroquinoline and related compounds of formula I and pharmaceutical compositions thereof, that exhibit useful antibacterial activity again a wide range of human and veterinary pathogens
Type:
Grant
Filed:
March 7, 2007
Date of Patent:
October 20, 2009
Assignee:
Pharmacia & Upjohn Company LLC
Inventors:
Michael Robert Barbachyn, J. Craig Ruble, Arthur Glenn Romero, Lisa Marie Thomasco, Alexander Ross Hurd, John Raymond Palmer, Peter Laurence Toogood, Dennis Joseph McNamara, Debra Ann Sherry, Paul Joseph Dobrowolski
Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
Type:
Application
Filed:
March 18, 2009
Publication date:
October 8, 2009
Inventors:
Francis Beaulieu, Carl Ouellet, B. Narasimhulu Naidu, Manoj Patel, Yasutsugu Ueda, Timothy P. Connolly, Jonathan R. Weiss, Michael A. Walker, Nicholas A. Meanwell, Kevin M. Peese, Margaret E. Sorenson
Abstract: A polymer that is a polysiloxane polymer has Levofloxacin groups, or pharmaceutically acceptable salts thereof, attached via linkers. The linkers may be hydrolytically labile thereby providing a manner of releasing the Levofloxacin from the polymer.
Type:
Application
Filed:
February 10, 2009
Publication date:
August 27, 2009
Inventors:
Shane Jeremy Stafslien, Bret Ja Chisholm, Alex J. Kugel
Abstract: The invention relates to substituted quinolones of formula (I) and to methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.
Type:
Grant
Filed:
December 28, 2007
Date of Patent:
August 4, 2009
Assignee:
AiCuris GmbH & Co. HK
Inventors:
Rudolf Schohe-Loop, Holger Zimmermann, Kerstin Henninger, Dieter Lang, Kai Thede, Chantal Fuerstner, David Brueckner
Abstract: The invention relates to [a]-fused indole compounds of the Formula II, or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein. The invention also relates to compositions comprising the compounds of Formula II, and methods for making and using the compounds.
Type:
Application
Filed:
January 30, 2009
Publication date:
July 30, 2009
Applicant:
Wyeth
Inventors:
Semiramis Ayral-Kaloustian, Nan Zhang, Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Thai Hiep Nguyen, James Thomas Anderson
Abstract: Described herein are antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.
Type:
Grant
Filed:
December 19, 2006
Date of Patent:
July 7, 2009
Assignee:
Pfizer Inc.
Inventors:
Timothy A. Johnson, Dennis J. McNamara, Debra A. Sherry, Peter Laurence Toogood
Abstract: This invention provides the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for treating or preventing heart failure. Particular heart disorders to be treated are selected from the group comprising chronic heart failure, congestive heart failure, chronic congestive heart failure and heart failure resulting from ischaemic heart disease. Methods of treating heart failure using 5-HT4 receptor antagonists and pharmaceutical compositions containing 5-HT4 receptor antagonists are also provided.
Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.
Abstract: The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.
Type:
Application
Filed:
November 26, 2008
Publication date:
June 25, 2009
Applicant:
pSivida, Inc.
Inventors:
Paul Ashton, Jianbing Chen, Hong Guo, Grazyna Cynkowska, Tadeusz Cynkowski
Abstract: The present invention relates to compounds having a structure according to Formula (I) wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
Type:
Application
Filed:
November 11, 2008
Publication date:
June 18, 2009
Inventors:
Benjamin Davis, Eugene B. Grant, III, Shu-Chen Lin, Mark J. Macielag, Michele Ann Weidner-Wells, Xiaoqing Xu, Xiaodong Xu, Bin Zhu
Abstract: A formulation for administration to the eye has at least one pharmaceutical agent such as a mydriatic agent, a cycloplegic agent, an anesthetic or a non-steroidal anti-inflammation agent combined with an anti-bacterial agent and a suitable carrier. The formulation can be made for topical or intracameral administration to the eye.
Abstract: The present invention is directed generally to a layered polymeric monofilament fiber drug delivery device, where each layer of the device can contain a different polymer, drug, additive, or any combination or mixture thereof. The layered nature of the current monofilament polymeric monofilament device provides the capability to modulate the release of one or more drugs and/or the mechanical properties of the fiber so that drug release and device failure can be separately tuned to provide for the tailored introduction of therapeutically effective drugs or agents to a target tissue. Moreover, the fiber may comprise more than one distinct segments along its length, each segment itself having different combinations and/or numbers of layers thereby providing even greater freedom in the design of the therapeutic delivery device. The invention is also directed to a method of manufacturing such a layered polymeric monofilament fiber drug delivery device, and methods of treatment using such devices.
Type:
Application
Filed:
November 12, 2008
Publication date:
June 18, 2009
Inventors:
Brendan C. Mack, Mark E. Davis, Kenneth W. Wright
Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.
Abstract: Novel modified release pharmaceutical compositions wherein the composition comprises at least one antibiotic(s) preferably amoxicillin or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof either alone or in combination with other antibiotic(s) as active ingredient, with at least one release modifying agent(s) for controlling the release of the beta lactam antibiotic optionally with one or more other pharmaceutically acceptable excipient(s) is provided, wherein the dosage form provides a release of not more than about 60% of the antibiotic in about 30 minutes and not less than about 70% of the antibiotic after 8 hours when subjected to in vitro dissolution study or when tested in vivo. Further, the compositions of the present invention which when tested in a group of healthy humans provide a mean peak plasma concentration (Cmax) after at least about 0.5 hour of administration of the dosage form.
Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.
Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R1, R2, R3 and R4 are independently selected from —H and halogen; X is selected from O, S, NR9 and CR9R10; R9 and R10 having different meanings; Y is selected from O, S, SO, SO2, NO, NR12 and CR12R13; R12 and R13 having different meanings. It also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections.
Type:
Application
Filed:
June 26, 2006
Publication date:
March 5, 2009
Applicant:
Ferrer Internacional, S.A.
Inventors:
Montserrat Cano, Albert Palomer, Antonio Guglietta
Abstract: The invention is intended for a treatment of severe infections using an injectable drug-delivery system comprising nanoparticles of a biodegradable polymer with incorporated antibacterial drug.
Type:
Application
Filed:
August 29, 2007
Publication date:
March 5, 2009
Inventors:
Joseph Schwarz, Michael Weisspapir, Hai Yan Gao
Abstract: The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
Type:
Application
Filed:
September 30, 2008
Publication date:
February 19, 2009
Inventors:
Abdellah TAHRI, Lili Hu, Dominique Louis Nestor Surleraux, Piet Tom Wigerinck
Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.
Type:
Application
Filed:
August 1, 2008
Publication date:
February 12, 2009
Applicant:
SANOFI-AVENTIS
Inventors:
Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
Abstract: The present invention relates to C-7 isoxazolyl quinoline/naphthyridine derivatives useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
Type:
Application
Filed:
July 28, 2008
Publication date:
January 29, 2009
Inventors:
Mark J. Macielag, Michele A. Weidner-Wells, Shu-Chen Lin
Abstract: This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.
Type:
Application
Filed:
July 7, 2006
Publication date:
January 29, 2009
Applicant:
BIO-MEDISINSK INNOVASJON AS
Inventors:
Jo Klaveness, Bjarne Brudeli, Finn Olav Levy
Abstract: The invention relates to pharmaceutical compositions comprising (i) a fluoroquinolone, (ii) a salt formed between a carboxylate anion and a divalent metal cation, (iii) a liquid comprising an organic solvent selected from the group consisting of glycerol, propylene glycol, glycerol formal, and (iv) optionally water. The invention further relates to methods of treating or preventing a condition in an animal comprising administering to the animal in need thereof a pharmaceutical composition of the invention.
Abstract: Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a nonionic polymer surfactant, such as an alkyl aryl polyether alcohol (e.g., tyloxapol) to the tympanic membrane. The medicaments delivered according to the methods of the invention include antibiotic, antiviral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.
Type:
Application
Filed:
August 25, 2006
Publication date:
December 25, 2008
Inventors:
William R. Campbell, Neil E. Paulsen, Roland H. Johnson
Abstract: The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
Type:
Grant
Filed:
April 11, 2006
Date of Patent:
December 16, 2008
Assignee:
Tibotec Pharmaceuticals Ltd.
Inventors:
Abdellah Tahri, Lili Hu, Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck
Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
Type:
Application
Filed:
July 15, 2008
Publication date:
November 13, 2008
Applicant:
Wyeth
Inventors:
Alexander Alexei Greenfield, Cristina Grosanu, Hassan Mahmoud Elokdah, Albert Jean Robichaud
Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
Type:
Application
Filed:
July 14, 2008
Publication date:
November 13, 2008
Applicant:
Wyeth
Inventors:
Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Cristina Grosanu, Albert Jean Robichaud
Abstract: Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a chemical penetration enhancer, such as propylene glycol. The compositions are applied to the ear so as to contact the outer surface of an intact tympanic membrane to deliver the medicament across the membrane and into the middle ear. The medicaments delivered according to the methods of the invention include antibiotic, anti-viral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.
Type:
Application
Filed:
August 24, 2006
Publication date:
October 30, 2008
Inventors:
William R. Campbell, Neil E. Paulsen, Roland H. Johnson
Abstract: The invention relates to substituted quinolones of formula (I) and to methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.
Type:
Application
Filed:
December 28, 2007
Publication date:
October 23, 2008
Inventors:
Rudolf Schohe-Loop, Holger Zimmermann, Kerstin Henninger, Dieter Lang, Kai Thede, Chantal Fuerstner, David Brueckner
Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor
Type:
Grant
Filed:
April 11, 2007
Date of Patent:
September 30, 2008
Assignee:
Wyeth
Inventors:
Alexander Alexei Greenfield, Cristina Grosanu, Hassan Mahmoud Elokdah, Albert Jean Robichaud
Abstract: The use is described of compounds of formula (I) wherein A is chosen from a phenyl or a heterocyclic ring with 5 or 6 members containing up to two heteroatoms chosen from nitrogen, oxygen and sulfur, X and Y represent carbon or nitrogen, and R1-R6 are as described in the specification, in the prevention and/or treatment of inflammatory and autoimmune diseases.
Type:
Application
Filed:
October 25, 2006
Publication date:
September 18, 2008
Applicant:
Brane Discovery S.r.l
Inventors:
Carlo Farina, Gabriela Constantin, Carlo Laudanna, Paola Misiano
Abstract: The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Abstract: The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a modified benzoxazine moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.
Abstract: The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
Type:
Application
Filed:
April 11, 2006
Publication date:
September 4, 2008
Inventors:
Abdellah Tahri, Lili Hu, Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck
Abstract: Methods of treating, preventing and/or managing a myelodysplastic syndrome are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and/or blood or cells for transplantation therapy. Specific second active ingredients are capable of affecting or improving blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Abstract: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.
Type:
Grant
Filed:
November 14, 2005
Date of Patent:
September 2, 2008
Assignee:
Bristol-Myers Squibb Company
Inventors:
B. Narasimhulu Naidu, Timothy P. Connolly, Yasutsugu Ueda