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46 results about "Chemokine Receptor Antagonist" patented technology

Any agent that binds to and blocks any of the chemokine receptor subtypes. Chemokine receptors, members of the G-protein coupled receptor family, are predominantly expressed on the surface of leukocytes and play an important role in inflammation, infectious diseases, and cancer.

Heterocylic antiviral compounds

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 R6c and X1 are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV-1) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treating diseases mediated by the CCR5 receptor.
Owner:ROCHE PALO ALTO LLC

Chemokine receptor antagonists and methods of use therefor

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and / or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: ##STR1## and physiologically acceptable salts thereof.
Owner:KYOWA HAKKO KOGYO CO LTD +1

Heterocyclic antiviral compounds

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
Owner:ROCHE PALO ALTO LLC

Piperazinylpiperidine derivatives as chemokine receptor antagonists

The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
Owner:INCYTE HLDG CORP

Chemokine receptor antagonists and methods of use thereof

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and / or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof
Owner:MILLENNIUM PHARMA INC +1

Heterocyclic antiviral compounds

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
Owner:ROCHE PALO ALTO LLC

Chemokine receptor antagonists

InactiveUS20020128307A1Low HIV-1-RNABiocideFungiTetramic acidChemokine Receptor Antagonist
Novel tetramic acid-type compounds isolated from a CCR-5 active complex produced by fermentation under controlled conditions of a biologically pure culture of the microorganism, Chaetomium globosum Kunze SCH 1705, ATCC 74489., pharmaceutical compositions containing the compounds and the use of the CCR-5 antagonist compounds and compositions to treat HIV-1 infections in humans are disclosed.
Owner:MERCK SHARP & DOHME CORP

Screening for CXCR4 receptor antagonism polypeptides for treating breast carcinoma and its uses

InactiveCN101334411AAbility to block transferHigh specific binding activityPeptide/protein ingredientsBiological testingLymphatic SpreadBinding site
The invention provides a screening and modification method, a marker and an application of polypeptide drugs which are used in the treatment of CXCR4 receptor-mediated breast cancer. A human chemokine SDF-1 Alpha and the homology region of a human herpes virus 8 MIP-II are compared, thereby obtaining a binding site of vMIP-II and CXCR4 receptor and further obtaining a CXCR4 specific binding active peptide. With the role of specific binding CXCR4 and the blocking of the physiological binding of the SDF-1 Alpha and the CXCR4, the CXCR4 specific binding active peptide is a high-efficient and specific chemokine receptor antagonist. The chemotactic activity of wide type SDF-1 Alpha to breast cancer cells and the growth of the breast cancer cells can be inhibited, and the growth and the metastasis of the CXCR4-positive tumor cells are simultaneously inhibited, thereby having the dual-target effect. The invention further provides a marked polypeptide to be targetedly positioned in sentinel lymph node and metastatic site, thereby being used in the detection and the targeted radiotherapy of the metastatic status of the sentinel lymph node before and in the operation of the breast cancer.
Owner:BENGBU MEDICAL COLLEGE

Chemokine receptor antagonists as therapeutic agents

The present invention provides methods and compositions to reduce immune tolerance at specific sites. In one aspect, the present invention comprises methods and compositions to reduce tumorigenicity. In an embodiment, the present invention reduces recruitment of tolerance-inducing antigen presenting cells (APCs) or their precursors to a tumor and / or tumor draining lymph node by decreasing binding of at least one tumor-associated ligand to a chemokine receptor present on the tolerance-inducing APCs or APC precursors. In an embodiment, the chemokine receptor is CCR6 and the tumor-associated ligand is mip-3α. In another aspect, the present invention comprises methods and compositions to reduce immune tolerance to a virus. In an embodiment, the virus is HIV. The present invention further provides for the development of CCR6 antibodies and antagonists as therapeutic agents to prevent or reduce immune tolerance.
Owner:GEORGIA HEALTH SCI UNIV RES INST

Methods of treating solid tumors with CCR2 antagonists

The present disclosure provides, inter alia, methods of treating a solid-tumor by administering an effective amount of a Chemokine Receptor 2 (CCR2) antagonist. Also provided herein are methods of reducing the number of macrophages in a solid tumor microenvironment, said method comprising administering effective amount of a Chemokine Receptor 2 (CCR2) antagonist. In an additional aspect, the current disclosure further provides methods of increasing the number CD8+ T cells in a solid tumor microenvironment, said method comprising administering effective amount of a Chemokine Receptor 2 (CCR2) antagonist. In some embodiments, the CCR2 antagonist has the formula I or Formula III:
Owner:RGT UNIV OF CALIFORNIA +1

Chemokine receptor antagonists and methods of use thereof

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and / or activation. The method comprises administering to a subject in need an effective amount of a compound represented by structural formula (I) or physiologically acceptable salt thereof.
Owner:MILLENNIUM PHARMA INC +1

Diagnostic biomarker to predict women at risk for preterm delivery

The invention relates to biomarkers associated with preterm delivery. More specifically, the invention provides methods of measuring biomarkers including but not limited to cytokines, cytokine receptors, cytokine receptor antagonists, chemokines, chemokine receptors, and / or chemokine receptor antagonists found in women that are at risk for preterm delivery. The diagnostic methods may be performed on whole blood.
Owner:CEDARS SINAI MEDICAL CENT

Functionalized heterocycles as chemokine receptor modulators

The present invention is a novel series of functionalized heterocycles as chemokine receptor modulators of Formula (I) useful as modulators of chemokine receptor activity. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the prepartion of the final products, pharmaceutical compositions containing the final products are also taught.
Owner:MILLENNIUM PHARMA INC

Octahydro-pyrrolo[3,4-c]pyrrole CCR5 receptor antagonists

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 and Ar are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
Owner:ROCHE PALO ALTO LLC

N-substituted heterocyclic amines as modulators of chemokine receptor activity

The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Owner:BRISTOL MYERS SQUIBB CO

Chemokine receptor antagonists and methods of use therefor

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and / or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
Owner:KYOWA HAKKO KIRIN CO LTD +1

Piperazinylpiperidine derivatives as chemokine receptor antagonists

The present invention relates to compounds of Formula I:wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
Owner:INCYTE HLDG CORP

Novel Combination of Compounds to be Used in the Treatment of Airway Diseases, Especially Chronic Obstructive Pulmonary Disease (COPD) and Asthma

The present invention relates to a combination of (a) a chemokine receptor 1 (CCR1) antagonist and (b) a muscarinic antagonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treatment of airway diseases, such as chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kit in treatment of airway diseases.
Owner:ASTRAZENECA AB

Chemokine receptor antagonists as therapeutic agents

The present invention provides methods and compositions to reduce immune tolerance at specific sites. In one aspect, the present invention comprises methods and compositions to reduce tumorigenicity. In an embodiment, the present invention reduces recruitment of tolerance-inducing antigen presenting cells (APCs) or their precursors to a tumor and / or tumor draining lymph node by decreasing binding of at least one tumor-associated ligand to a chemokine receptor present on the tolerance-inducing APCs or APC precursors. In an embodiment, the chemokine receptor is CCR6 and the tumor-associated ligand is mip-3α. In another aspect, the present invention comprises methods and compositions to reduce immune tolerance to a virus. In an embodiment, the virus is HIV. The present invention further provides for the development of CCR6 antibodies and antagonists as therapeutic agents to prevent or reduce immune tolerance.
Owner:MUNN DAVID H +2

Antagonists of chemokine receptors

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
Owner:CHEMOCENTRYX INC

Methods of treating solid tumors with ccr2 antagonists

The present disclosure provides, inter alia, methods of treating a solid-tumor by administering an effective amount of a Chemokine Receptor 2 (CCR2) antagonist. Also provided herein are methods of reducing the number of macrophages in a solid tumor microenvironment, said method comprising administering effective amount of a Chemokine Receptor 2 (CCR2) antagonist. In an additional aspect, the current disclosure further provides methods of increasing the number CD8+ T cells in a solid tumor microenvironment, said method comprising administering effective amount of a Chemokine Receptor 2 (CCR2) antagonist. In some embodiments, the CCR2 antagonist has the formula I:
Owner:RGT UNIV OF CALIFORNIA +1

Solid forms of a chemokine receptor antagonist and methods of use thereof

The citrate salt of (S)-4-(4-Chloro-phenyl)-1-{3-[7-(1-hydroxy-1-methyl-ethyl)-11H-10-oxa-1-aza-dibenzo[a,d]cyclohepten-5-ylidene]-propyl}-3,3-dimethyl-piperidin-4-ol, which may be used in pharmaceutical applications, is disclosed. The crystalline Citrate Salt, including particular single crystal forms and combinations of the single crystalline forms, are also discussed. Mixtures for forming the crystalline salts are discussed. As well, methods of producing the Citrate Salt, and crystalline forms thereof, and using such Citrate Salt, and crystalline forms thereof, in treating diseases associated with aberrant leukocyte recruitment, activation, or recruitment and activation are also discussed.
Owner:MILLENNIUM PHARMA INC

Antagonists of chemokine receptors

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
Owner:CHEMOCENTRYX INC
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