31 results about "Ccr2 antagonist" patented technology

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.

Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Anti-MCP-1 / CCR2 antagonist therapy is provided for the control or reversal of fibrosis related diseases, including, e.g., but not limited to MCP-1 / CCR2 antagonist therapy for the modulation of profibrotic markers associated with fibrotic processes including collagen matrix deposition and alveolar collapse.

Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.

Myeloid derived suppressor cell (MDSC) inhibitory agents and vaccine and / or adjuvant enhancers are provided. Improved vaccine treatment regimens employing these agents are also provided. Cancer vaccines and methods for inhibiting tumor growth and cancer metastases are also presented. The myeloid derived suppressor cell (MDSC) inhibiting agents are described as bisphosphonates (such as liposomal clodronate) and CCR2 inhibitors and / or CCR2 antagonists. Methods for enhancing antibody titer levels in response to an antigen of interest are also provided.

The present invention is concerned with novel processes for the preparation of (R)-4,4-dimethoxy-pyran-3-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity including CCR2 antagonists.

The invention relates to a novel CCR2 antagonist and an application thereof. Specifically, the invention discloses an application of a compound as shown in formula I (referring to the Description) or pharmaceutically acceptable salt in preparing medicines or reagents for regulating tumor microenvironment, relieving aggregation of macrophage or bone marrow cells towards primary tumors, inhibiting tumor growth, inhibiting angiogenesis and / or increasing CD8T cells in a required object, as well as an application in preparing medicines for preventing or treating CCR2-mediated diseases in the object or an application in preparing medicines or reagents for inhibiting a CCR2 or CCL2-CCR2 pathway, wherein in the formula, a, b, c, d, R1, R2, R3 and R4 are as described in the Description.

Provided herein are methods of treating focal segmental glomerulosclerosis, said methods include administering to a subject in need thereof a therapeutically effective amount of a CCR2 antagonist. In some embodiments, the CCR2 antagonist is used in monotherapy. In some embodiments, the CCR2 antagonist is used in combination therapy. In some embodiments, the additional therapeutic agent is a RAAS blocker and / or an endothelin receptor inhibitor. The CCR2 antagonist may have the structure of formula (I).

A method of treating liver fibrosis with CCR2 antagonists is provided. The liver fibrosis may be associated with non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), emerging cirrhosis, non-cirrhotic hepatic fibrosis, type 2 diabetes mellitus (T2DM) or metabolic syndrome (MS).

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:

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:

The innovation is directed to a method for treating a CCR5 and / or CCR2 mediated disease such as nonalcoholic steatohepatitis (NASH) comprising administering an effective amount of a C—C Chemokine receptor 5 (CCR5) antagonist (e.g., maraviroc or vicriviroc or cenicriviroc) and / or an effective amount of a C—C Chemokine receptor 2 (CCR2) antagonist, or a CCR5 / CCR2 antagonist together with an effective amount of farnesoid X receptor (FXR) agonist (e.g., obeticholic acid (OCA)). An “effective amount” can be a regular clinical dose of either agent alone or a reduced dose of the FXR receptor agonist and / or the CCR5 / CCR2 antagonist. The combination is effective to treat NASH with (1) enhanced efficacy and (2) substantial reduction of side effects, particularly those associated with administration of OCA or its analogues, namely less effect on liver enzyme elevation, and less severity and frequency of pruritus (3). The fixed dose combination provides for better efficacy and safety profile.

The innovation is directed to a method for treating a CCR5 and / or CCR2 mediated disease such as nonalcoholic steatohepatitis (NASH) comprising administering an effective amount of a C-C Chemokine receptor 5 (CCR5) antagonist (e.g., maraviroc or vicriviroc or cenicriviroc) and / or an effective amount of a C-C Chemokine receptor 2 (GGR2) antagonist, or a CCR5 / CCR2 antagonist together with an effective amount of farnesoid X receptor (FXR) agonist (e.g., obeticholic acid (OCA)). An effective amount can be a regular clinical dose of either agent alone or a reduced dose of the FXR receptor agonist and / or the CCR5 / CCR2 antagonist. The combination is effective to treat NASH with (1) enhanced efficacy and (2) substantial reduction of side effects, particularly those associated with administration ofOCA or its analogues, namely less effect on liver enzyme elevation, and less severity and frequency of pruritus (3). The fixed dose combination provides for better efficacy and safety profile.