Abstract: A compound of formula (I)
and salts and solvates thereof, in which:
R0 represents hydrogen, halogen or C1-6 alkyl;
R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, haloC1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl or heteroarylC1-3alkyl;
R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring
attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and
R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain.
Abstract: A fermentation process post-sterile additive device and method of operation is detailed. The device is used to deliver additive as a heavy-drop mist. The mist covers the entire fermenting batch head surface of the vat broth. This improves mixing and reduces the amount of additive to appropriate introduction levels throughout log phase fermentation, preventing coating of cultivating cells and interference with cell respiration. A steady state growth rate is fostered.
Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract: The present invention provides novel human PDE10 polypeptides, polynucleotides encoding the polypeptides, expression constructs comprising the polynucleotides, host cells transformed with the expression constructs; methods for producing PDE10 polypeptides; antisense polynucleotides; and antibodies specifically immunoreactive with the PDE10 polypeptides. The invention further provides methods to identify binding partners of PDE10, and more particularly, binding partners that modulate PDE10 enzyme activity.
Abstract: Novel compounds that are potent and selective inhibitors of PIDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
February 19, 2002
Assignee:
ICOS Corporation
Inventors:
Kerry W. Fowler, Amy Oliver, Joshua Odingo
Abstract: DNA sequences encoding seven novel seven transmembrane receptors and variants thereof are disclosed as well as materials and methods for production of the same by recombinant techniques. Antibody substances specific for each of the seven transmembrane receptors are disclosed as useful for the modulation of the ligand/receptor binding reactions of the receptors.
Type:
Grant
Filed:
June 1, 1998
Date of Patent:
February 19, 2002
Assignee:
ICOS Corporation
Inventors:
Ronald Godiska, Patrick W. Gray, Vicki Louise Schweickart
Abstract: Polynucleotides encoding novel Atr-2 cell cycle checkpoint polypeptides are disclosed, along with expression constructs comprising the polynucleotides, host cells transformed with the expression constructs, methods to make the Atr-2 polypeptides using the host cells, Atr-2 polypeptides, and binding partners of the Atr-2 polypeptides.
Abstract: The present invention provides purified and isolated polynucleotide sequences encoding a novel human macrophage-derived C-C chemokine designated MDC. Also provided are materials and methods for the recombinant production of the chemokine, and purified and isolated chemokine protein.
Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract: Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3′,5′-monophoshate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of therapeutic areas where such inhibition is thought to be beneficial, including the treatment of cardivascular disorders.
Abstract: DNA sequences encoding a novel human intercellular adhesion molecule polypeptide (designated “ICAM-R”) and variants thereof are disclosed along with methods and materials for production of the same by recombinant procedures. Binding molecules specific for ICAM-R and variants thereof are also disclosed as useful in both the isolation of ICAM-R from natural cellular sources and the modulation of ligand/receptor binding biological activities of ICAM-R.
Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract: The present invention provides purified and isolated polynucleotide sequences encoding human plasma platelet-activating factor acetylhydrolase. Also provided are materials and methods for the recombinant production of platelet-activating factor acetylhydrolase products which are expected to be useful in regulating pathological inflammatory events.
Type:
Application
Filed:
December 4, 2000
Publication date:
September 13, 2001
Applicant:
ICOS Corporation
Inventors:
Lawrence S. Cousens, Christine D. Eberhardt, Patrick Gray, Hai Le Trong, Larry W. Tjoelker, Cheryl L. Wilder
Abstract: The present invention provides polynucleotides that encode the chemokine receptors 88-2B or 88C and materials and methods for the recombinant production of these two chemokine receptors. Also provided are assays utilizing the polynucleotides which facilitate the identification of ligands and modulators of the chemokine receptors. Receptor fragments, ligands, modulators, and antibodies are useful in the detection and treatment of disease states associated with the chemokine receptors such as atherosclerosis, rheumatoid arthritis, tumor growth suppression, asthma, viral infection, AIDS, and other inflammatory conditions.
Type:
Grant
Filed:
June 7, 1996
Date of Patent:
July 31, 2001
Assignee:
Icos Corporation
Inventors:
Patrick W. Gray, Vicki L. Schweickart, Carol J. Raport
Abstract: The present invention provides polynucleotides that encode the chemokine receptors 88-2B or 88C and materials and methods for the recombinant production of these two chemokine receptors. Also provided are assays utilizing the polynucleotides which facilitate the identification of ligands and modulators of the chemokine receptors. Receptor fragments, ligands, modulators, and antibodies are useful in the detection and treatment of disease states associated with the chemokine receptors such as atherosclerosis, rheumatoid arthritis, tumor growth suppression, asthma, and other inflammatory conditions.
Type:
Grant
Filed:
December 20, 1995
Date of Patent:
July 24, 2001
Assignee:
Icos Corporation
Inventors:
Patrick W. Gray, Vicki L. Schweickart, Carol J. Raport
Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Grant
Filed:
December 23, 1999
Date of Patent:
July 10, 2001
Assignee:
ICOS Corporation
Inventors:
Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlacter
Abstract: The present invention relates generally to a novel CREBa polypeptide isoform, polynucleotides encoding the polypeptide, expression constructs comprising the polynucleotides, host cell transformed or transfected with the polynucleotides, methods for producing the polypeptide, and methods to identify inhibitors of binding between the CREBa and other polypeptides or polynucleotides.
Abstract: A compound of formula
and salts and solvates thereof, wherein R0, R1, and R2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.
Type:
Grant
Filed:
August 24, 1999
Date of Patent:
April 17, 2001
Assignee:
ICOS Corporation
Inventors:
Alain Claude-Marie Daugan, Richard Frederic LaBaudiniere
Abstract: The present invention provides purified and isolated polynucleotides encoding IRP (Integrin Regulatory Protein) polypeptides which regulate &bgr;2 and &bgr;7 integrins and which are contemplated to participate in integrin signaling and/or recycling pathways. Also provided are methods for identifying modulators of IRP activities and methods for identifying other proteins which interact with IRP polypeptides in signaling pathways. Modulators of IRP interactions are contemplated to be useful, for example, in monitoring and treating inflammatory processes involving leukocytes.