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Although this SAR strategy is highly controllable but if a series of compounds are less active, or if the molecular skeleton of this series is less efficient, then you take such a small step to improve to find a drug-level compound to get the Year of the Monkey.
this is like you go to the second ring to find auspicious hutong A 5, only you have to auspicious hutong door by door to find is more reasonable.
if you're still outside the six rings and you start looking door-to-door, it's too inefficient, you can drive at high speed at least 30km away.
drug chemistry has a saying called methyl, ethyl, propyl, futile, that's what it means.
This solution in the pharmaceutical chemistry of the corresponding technology is called skeleton migration, and SAR methyl, ethyl, propylene knock on the door, skeleton migration significantly change the molecular skeleton, in the hope of biological activity has a larger change.
Of course, molecular skeleton changes can have a significant negative impact on biological activity in most cases, but occasionally there will be a large positive impact on the transformation, and then you have a new skeleton, which may open up new opportunities.
some computational techniques may help with system modifications, and it is more effective to know the structure of protein crystals.
simple analogoons of morphine-like drugs such as fentanine, which is now being abused badly, could be an early example.
new use of old drugs can be counted as the study of the adaptive-active relationship, that is, the same molecular structure in different biological testing system activity is different.
similar to SARS is the expansion of adaptive disorders in the same disease, such as the expansion of PD-1 drugs from evil black to lung, stomach, liver and other similar tumors.
it is relatively easy to expand this adaptive disease, so usually the original research manufacturers will be fully developed.
chances of developing later stages are relatively small, there are examples of Imfinzi's occupation of stage III lung cancer.
the dramatic changes in adaptive disorders, from controlling pregnancy responses to multiple myeloma, are similar to drug-chemical skeleton migrations, and finding this new adaptation is more valuable and, of course, more technically difficult.
this additional difficulty makes the original research manufacturers and competitors basically stand at the same starting point, so the development of preferred adaptive backward manufacturers if they have the ability to find irrelevant adaptive disorders, then began a new competition.
new use of old drugs is much more complex than skeleton migration, from EGFR variation to the expansion of the EGFR wild population may be a problem, not to mention take sugar-lowering drugs to treat heart failure.
esolying is now a common technique, but esothype changes alone are not enough and need to be supported by other supporting evidence.
clinical stumbles are an important source, such as the famous Viagra event, but this requires clinicians to be vigilant at all times and is not easy in today's full-time environment.
But the discovery of this new adaptive disorder has great commercial value, in addition to reaction stop, CD20 antibodies from CLL to MS, fumarate from psoriasis to MS make simple structure, the preferred adaptive performance mediocre or even catastrophic (such as reaction stop) drugs become heavy drugs.
With the exponential growth of high-quality compounds targeted at new targets, and the opportunities for new drugs across diseases ("adaptation leaps"), the industry should consider appropriate investors to establish evaluation facilities and theoretical technical support.
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