CXCR7 Receptor Modulators Overcoming Tumor Resistance

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Solution Overview

Problem

Current cancer treatments face challenges due to tumor resistance mechanisms involving the CXCL12 pathway, particularly the CXCR7 receptor, which promotes cancer cell survival, invasion, and metastasis, limiting the effectiveness of conventional therapies.

Innovation Solution

Development of novel CXCR7 receptor modulators, including compounds of formula (I), which act as agonists or antagonists to target and modulate the CXCR7 receptor, potentially sensitizing cancer cells to existing therapies and inhibiting tumor growth and metastasis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer therapies are used, then treatment is administered with standard protocols, but tumor resistance develops due to CXCR7 receptor activation limiting therapeutic effectiveness

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidtumor resistance

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary anti-action by administering CXCR7 receptor modulators before or in combination with conventional cancer therapies to prevent tumor resistance from developing. The modulators block the CXCR7 receptor pathway that tumors use to resist chemotherapy and radiotherapy, thereby preemptively counteracting the resistance mechanism before it can limit therapeutic effectiveness

Inventive Principle:

Principle #9Preliminary anti-action

Solution Approach 2:

The patent uses CXCR7 receptor modulators as an intermediary substance that mediates between the conventional therapy and the tumor cells. The modulator binds to the CXCR7 receptor on tumor cells, blocking the harmful signaling pathway while allowing the conventional therapy to exert its effect, thus enhancing overall therapeutic effectiveness without directly replacing the standard treatment

Inventive Principle:

Principle #24Intermediary (Mediator)

2Strength

If CXCR7 receptor is activated by CXCL12, then cancer cell survival and invasion are promoted, but this limits the effectiveness of chemotherapy and radiotherapy

Engineering Contradiction:

Improvecancer cell survivalVSAvoidtreatment effectiveness

Core Design Contradiction:

StrengthVSReliability

Solution Approach 1:

The patent applies preliminary anti-action by blocking the CXCR7 receptor with modulators before chemotherapy or radiotherapy is administered. This prevents the receptor from receiving survival signals from CXCL12, thereby preemptively reducing cancer cell survival capacity and sensitizing the cells to the subsequent conventional therapy

Inventive Principle:

Principle #9Preliminary anti-action

Solution Approach 2:

The patent converts the harmful effect of CXCR7 activation into a benefit by using modulators that target this pathway. The same receptor pathway that promotes tumor survival and resistance is now being exploited as a therapeutic target, where blocking it enhances treatment effectiveness and overcomes resistance mechanisms

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentUS9920010B2CXCR7 receptor modulators

Publication Date: 2018.03.20 IDORSIA PHARMACEUTICALS LTD

AI summary

The present invention relates to derivatives of formula (I)wherein (R1)n, R2a, R2b, R3a, R3b, R4, L1, L2, X, Y and Ar1 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.