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1
US7157469B2
Publication/Patent Number: US7157469B2
Publication date: 2007-01-02
Application number: 11/416,004
Filing date: 2006-05-02
Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same. Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and ...more ...less
2
US7157472B2
Publication/Patent Number: US7157472B2
Publication date: 2007-01-02
Application number: 10/609,638
Filing date: 2003-06-30
Abstract: The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of ...more ...less
3
US7157488B2
Publication/Patent Number: US7157488B2
Publication date: 2007-01-02
Application number: 10/472,741
Filing date: 2002-03-15
Abstract: The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I. The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with ...more ...less
4
US7157085B2
Publication/Patent Number: US7157085B2
Publication date: 2007-01-02
Application number: 10/791,619
Filing date: 2004-03-02
Abstract: The present invention relates to a method for adjusting the affinity of a polypeptide to a target molecule by a combination of steps, including: (1) the identification of aspartyl residues which are prone to isomerization; (2) the substitution of alternative residues and screening the resulting mutants for affinity against the target molecule. In a preferred embodiment, the method of subtituting residues is affinity maturation with phage display (AMPD). In a further preferred embodiment the polypeptide is an antibody and the target molecule is an antigen. In a further preferred embodiment, the antibody is anti-IgE and the target molecule is IgE. In another embodiment, the invention relates to an anti-IgE antibody having improved affinity to IgE. The present invention relates to a method for adjusting the affinity of a polypeptide to a target molecule by a combination of steps, including: (1) the identification of aspartyl residues which are prone to isomerization; (2) the substitution of alternative residues and ...more ...less
5
US7157089B1
Publication/Patent Number: US7157089B1
Publication date: 2007-01-02
Application number: 08/977,787
Filing date: 1997-11-25
Abstract: The present invention relates to a vaccine for inducing an immune response to an antigen in a vertebrate (e.g., mammal) comprising an antigen and all or a portion of a stress protein or all or a portion of a protein having an amino acid sequence sufficiently homologous to the amino acid sequence of the stress protein to induce the immune response against the antigen. In a particular embodiment, the present invention relates to vaccines and compositions which induce a CTL response in a mammal comprising an antigen and all or a portion of a stress protein. In another embodiment, the invention relates to vaccines and compositions which induce an immune response to an influenza virus in a mammal comprising an antigen of the influenza virus and all or a portion of one or more stress proteins. The invention also relates to vaccines and compositions for inducing a CTL response to a tumor-associated antigen comprising a tumor-associated antigen and all or a portion of the stress protein. The invention also relates to vaccines and composition for suppressing allergic immune responses to allergens comprising an allergen and all or a portion of a stress protein. The present invention relates to a vaccine for inducing an immune response to an antigen in a vertebrate (e.g., mammal) comprising an antigen and all or a portion of a stress protein or all or a portion of a protein having an amino acid sequence sufficiently homologous to the ...more ...less
6
US7157091B1
Publication/Patent Number: US7157091B1
Publication date: 2007-01-02
Application number: 09/336,091
Filing date: 1999-06-18
Abstract: The invention provides isolated HLA DRB1*15-binding peptides consisting of the amino acid sequence set forth as SEQ ID NO:7 with 0–10 amino acids added to either or both ends of the amino acid sequence set forth as SEQ ID NO:7, and an endosomal targeting signal comprising an endosomal targeting portion of human invariant chain Ii or LAMP-1. The invention provides isolated HLA DRB1*15-binding peptides consisting of the amino acid sequence set forth as SEQ ID NO:7 with 0–10 amino acids added to either or both ends of the amino acid sequence set forth as SEQ ID NO:7, and an endosomal targeting signal comprising ...more ...less
7
US7157095B2
Publication/Patent Number: US7157095B2
Publication date: 2007-01-02
Application number: 10/211,682
Filing date: 2002-08-02
Abstract: An anti-fungal product is comprised of at least three delayed release dosages forms, each of which has a different release profile, with the Cmax for the anti-fungal product being reached in less than about twelve hours after initial release of anti-fungal from the product.
8
US7157103B2
Publication/Patent Number: US7157103B2
Publication date: 2007-01-02
Application number: 10/214,410
Filing date: 2002-08-06
Inventor: Sackler, Richard  
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.
9
US7157104B1
Publication/Patent Number: US7157104B1
Publication date: 2007-01-02
Application number: 10/444,470
Filing date: 2003-05-27
Assignee: Zenitech LLC
Abstract: The present invention relates to Cranberry seed oil derivatives derived by the reaction of a guerbet alcohol and cold pressed Cranberry seed oil. The choice of cold pressed Cranberry seed oil as a raw material in the preparation of the compounds of the present invention is critical, since it has been found that the cold pressed Cranberry seed oil contains antioxidants, antimicrobial compounds and which when reacted with a guerbet alcohol result in products that deliver said actives to the skin and hair, resulting in protection of the skin and hair from environmental factors such as acid rain, ozone attack and UV degradation. The present invention relates to Cranberry seed oil derivatives derived by the reaction of a guerbet alcohol and cold pressed Cranberry seed oil. The choice of cold pressed Cranberry seed oil as a raw material in the preparation of the compounds of the present invention is ...more ...less
10
US7157108B2
Publication/Patent Number: US7157108B2
Publication date: 2007-01-02
Application number: 10/148,976
Filing date: 2000-12-11
Abstract: The invention relates to dried milk protein concentrates and their use. In particular the invention relates to such dried concentrates which have been calcium-depleted to an extent which allows improvements in the use of dried milk protein concentrates in cheese manufacture. The invention includes a method of cheese manufacture comprising: (a) dispersing in milk a dried MPC or MPI having at least 70% dry matter as milk protein; (b) treating the resulting mixture with one or more coagulating enzymes to produce a curd; and (c) processing the curd to make cheese; wherein the dried MPC or MPI is a calcium-depleted MPCF or MPI and the extend of calcium depletion is sufficient to allow manufacture of substantially nugget-free cheese. The invention relates to dried milk protein concentrates and their use. In particular the invention relates to such dried concentrates which have been calcium-depleted to an extent which allows improvements in the use of dried milk protein concentrates in cheese manufacture. The ...more ...less
11
US7157110B2
Publication/Patent Number: US7157110B2
Publication date: 2007-01-02
Application number: 10/436,505
Filing date: 2003-05-12
Abstract: Fat compositions that contain a vegetable oil and a plant-derived wax component are described. Food and cosmetic products containing such fat compositions also are described.
12
US7157127B2
Publication/Patent Number: US7157127B2
Publication date: 2007-01-02
Application number: 10/753,573
Filing date: 2004-01-08
Inventor: Schmelzer, Winfried  
Abstract: A label for adhesive attachment to a stack of articles combined by an exterior substrate. The label includes a label material having a pair of outer label regions, a central label region, a signal surface having indications and an adhesive surface, the adhesive surface being provided with an adhesive. The label also includes a protective release cover, wherein the release cover is releasably attached to the adhesive surface of the label. The release cover also includes at least two separating lines, wherein the separating lines divide the release cover into two outer regions separated by a center region such that the regions of the release cover can be removed from the label material independently from each other. A label for adhesive attachment to a stack of articles combined by an exterior substrate. The label includes a label material having a pair of outer label regions, a central label region, a signal surface having indications and an adhesive surface, the adhesive surface being ...more ...less
13
US7157140B1
Publication/Patent Number: US7157140B1
Publication date: 2007-01-02
Application number: 10/792,474
Filing date: 2004-03-03
Inventor: Hoppe, Karl M.  
Assignee: RTP Company
Abstract: Malleable thermoplastic composite materials are provided. More specifically, malleable thermoplastic composite materials made from thermoplastic polymers having low molecular weight and particulate material are provided for malleable composites having high compression set. Alternatively, malleable composite blends of two or more thermoplastic polymers are provided wherein at least one thermoplastic polymer has a low molecular weight. Further, the malleable thermoplastic composites may be blended with high specific gravity particulate material to form high specific gravity composites that exhibit malleable characteristics. Malleable thermoplastic composite materials are provided. More specifically, malleable thermoplastic composite materials made from thermoplastic polymers having low molecular weight and particulate material are provided for malleable composites having high compression set ...more ...less
14
US7157414B2
Publication/Patent Number: US7157414B2
Publication date: 2007-01-02
Application number: 10/922,669
Filing date: 2004-08-19
Abstract: Provided are methods of reducing the irritation associated with a personal care composition comprising an anionic surfactant, the methods comprising combining a hydrophobically-modified material capable of binding a surfactant thereto with an anionic surfactant to produce a reduced irritation personal care composition, and methods of using such compositions to cleanse the hair or skin with reduced irritation. Provided are methods of reducing the irritation associated with a personal care composition comprising an anionic surfactant, the methods comprising combining a hydrophobically-modified material capable of binding a surfactant thereto with an anionic surfactant to produce a ...more ...less
15
US7157416B2
Publication/Patent Number: US7157416B2
Publication date: 2007-01-02
Application number: 10/333,176
Filing date: 2001-07-20
Abstract: Enzyme-containing formulations having improved stability and enzymatic activity in liquid medium, comprising one or more protease enzymes produced from any Bacillus bacteria, at least about 5% alkali metal halide salt, and at least about 50% polyol. Also disclosed are methods for making such formulations. Enzyme-containing formulations having improved stability and enzymatic activity in liquid medium, comprising one or more protease enzymes produced from any Bacillus bacteria, at least about 5% alkali metal halide salt, and at least about 50% polyol. Also disclosed are methods ...more ...less
16
US7157422B2
Publication/Patent Number: US7157422B2
Publication date: 2007-01-02
Application number: 10/810,578
Filing date: 2004-03-29
Abstract: Peptide inhibitors of glycogen synthase kinase-3 (GSK-3) having an amino acid sequence motif of XZXXXS(p)X, wherein S(p)=phosphorylated serine or phosphorylated threonine, X=any amino acid, and Z=any amino acid except serine or threonine. These inhibitors, which are about 7 to 20 amino acids long, are specific for GSK-3 and strongly inhibit the enzyme with an IC50 of about 150 μM. Also provided are methods of treating biological conditions mediated by GSK-3 activity, such as potentiating insulin signaling in a subject, treating or preventing type 2 diabetes in a patient, and treating Alzheimer's Disease by administering peptide inhibitors. Compositions of these peptide inhibitors and pharmaceutically acceptable carriers are also provided, as is a method for identifying inhibitors of GSK-3. The invention further relates to a computer-assisted method of structure based drug design of GSK-3 inhibitors using a three-dimensional structure of a peptide substrate of GSK-3. Peptide inhibitors of glycogen synthase kinase-3 (GSK-3) having an amino acid sequence motif of XZXXXS(p)X, wherein S(p)=phosphorylated serine or phosphorylated threonine, X=any amino acid, and Z=any amino acid except serine or threonine. These inhibitors, which are about 7 to ...more ...less
17
US7157424B2
Publication/Patent Number: US7157424B2
Publication date: 2007-01-02
Application number: 10/807,023
Filing date: 2004-03-23
Abstract: Disclosed are pharmaceutical compositions of hepatitis C viral protease inhibitors, and methods of using these compositions for inhibiting the replication of the hepatitis C virus (HCV) and for the treatment of an HCV infection. These compositions are lipid based systems and comprise the hepatitis C viral protease inhibitor together with at least one pharmaceutically acceptable amine, at least one pharmaceutically acceptable base, at least one pharmaceutically acceptable oil and optionally one or more additional ingredients. Disclosed are pharmaceutical compositions of hepatitis C viral protease inhibitors, and methods of using these compositions for inhibiting the replication of the hepatitis C virus (HCV) and for the treatment of an HCV infection. These compositions are lipid based systems and ...more ...less
18
US7157427B2
Publication/Patent Number: US7157427B2
Publication date: 2007-01-02
Application number: 10/809,761
Filing date: 2004-03-25
Abstract: Anti-bacterial peptides are provided which are derived from the bacteriophage SPO1.
19
US7157438B2
Publication/Patent Number: US7157438B2
Publication date: 2007-01-02
Application number: 10/049,502
Filing date: 2001-06-18
Inventor: Sebti, Said M.  
Abstract: The protein RhoB and its variants as a supressor of cancer cell growth, inhibitor of malignant cell transformation, and modulator of oncogenic signaling, wherein introducing RhoB directly, or indirectly via a nucleic acid, into a malignantly transformed cell or a cancerous cell decreases phosphorylation of Erk and Akt proteins inhibiting the PI3-kinase/Akt cell survival pathway and promoting apoptotic cell death. Methods and compositions are disclosed for administering to cancer patients, a prophylactic treatment to minimize the risk of malignant transformation, and advantageous combination of RhoB therapy with existing cancer treatments. The protein RhoB and the variants of the present invention are prenylated with either geranylgeranyl or farnesyl, and provision is made for selection of the prenylating moiety. The protein RhoB and its variants as a supressor of cancer cell growth, inhibitor of malignant cell transformation, and modulator of oncogenic signaling, wherein introducing RhoB directly, or indirectly via a nucleic acid, into a malignantly transformed cell or a cancerous cell ...more ...less
20
US7157440B2
Publication/Patent Number: US7157440B2
Publication date: 2007-01-02
Application number: 10/855,471
Filing date: 2004-05-27
Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.