Member Info for sadoldgit

Once the realisation of the importance of patent protection of our compounds are realised, by the interested parties then the doors are now wide open for serious discussions. A formal offer for on license now cannot be far off.

Regards

Hi Stoney40. Good post from you. A concern you have of individually tailored treatments is of great importance. We are at a stage whereby targeted kinase inhibitors are reaching a potential way in advance of what was once thought.

We now have 17 years of protection.
Molecules can be tweaked to maximise inhibition in an effort to achieve maximum safety and at the same time effectiveness, i dare say our SKIL played a vital part in this,

I was also intrigued at the level of new information in areas critical to certain targets.

One size does not fit all, and my belief that due to lack selectivity and not paying attention to detail in the areas of qulity control is the reason many inhibitors have fallen by the wayside at great expense to a financially committed pharma.

A new world is dawning with targeted kinase inhibitors especially Tyk 2 ( not the be all and end all on its own)

We will be at the forefront of that I am sure. Attention to detail whilst hard at times will I perceive pay off.

Both SDC1801 and 1802 have a potential to rake in many tens of billions in revenue over the next 17 years.

Of most importance is lives will be saved and the quality of life for many will change for the better too.

Regards

FWIIW my opinion is, should any other party use these patent protected methods for the furtherment of their own compounds, then yes a royalty either as a percentage or one off payment shall be made.
You are looking at X ray crystallography for one example ( whilst not new) is is utilised here to determine the purity of a compound. Even pertaining to the angular degrees to measure peaks at specified angles to confirm compound integrity.

This is my take on it. Sareum had problems with SDC1802 new patent ( as considered too similar to 1801) the god damn mothers would not on repeat applications grant a new patent. However. it would appear that Mr Reader has worked a blinder here in protecting the compound not as the compound per se. but in the manufacture and methods used in quality control ie levels of purity thereof.

In this instance you cannot verify the quality of the compound ( lack of impurities) unless these methods of quality control are provided. It is indeed very complex and precise.

It does also allow further compounds to be made from the molecules which in themselves have patent protection.

In a nutshell we have secured patent protection to allow an extremely high level of quality ( minimalisation of impurities with their associated affects in toxicity and effectiveness ) in the manufacture of our compounds.

Any other party wishing to use this route, or similar to, would be treading on dodgy ground risking patent infringement.

Regards

One more thing I will add and I will then sod off and leave you all in peace. This protects SDC1801 and SDC1802 compounds. The door is now well and truly opened to 'on licensing'. Patent protection for 17 years of Sareums compounds with the added bonus of royalties should another party use this method in the manufacture and quality control of their own products.

Regards

Before offers are made, in whichever form, the period of patent protection provided to its invention ( in this case the manufacture and quality control of its compounds) needs to be realised and confirmed. A very major milestone achieved.

Regards

Taken from the patent.
The invention provides crystalline forms of a compound having the formula (I) along with methods of making the crystalline forms and pharmaceutical formulations comprising the crystalline forms.
Two areas relevant.
"X"
document of particular relevance; the claimed invention cannot be considered novel or cannot be considered to involve an inventive step when the document is taken alone'

However, it is not alone.

P"
document published prior to the international filing date but later than the priority date claimed.

As far as I can see it effectively gives our TYk 2 compounds and looks like Aurora +FLT+3 too, a17 year patent protection from the 26th of October 2021.

Regards

Masses of patent protection to its compounds in formulation and derivation.

The Invention

It has now been found that the compound of formula (1), 2-(2,6-dichlorophenyl)-5-[4-(1,1-dioxo-1,4-thiazinane-4-carbonyl)anilino]oxazole-4-carboxamide, can form several different crystalline forms.

Accordingly, in a first embodiment (Embodiment 1.0), the invention provides a substantially crystalline form of a compound having the formula (1):

The crystalline form can be, for example, any one of crystalline forms A, B, C and D as defined herein.

The above compound may be referred to herein variously as “a compound having the formula (1)”, “the compound of formula (1)”, “compound (1)”, “compound of the formula (1)”, “Compound (1)” or “a compound of the invention”, or like terms, and these terms are used herein as synonyms.

In an amorphous solid, the three-dimensional structure that normally exists in a crystalline form does not exist and the positions of the molecules relative to one another in the amorphous form are essentially random, see for example Han**** etal. J. Pharm. Sci. (1997), 86, 1).

The term “substantially crystalline” refers to forms of the compound of formula (1) in which it is from 50% to 100% crystalline. Within this range, the compound of formula (1) may be at least 55% crystalline, or at least 60% crystalline, or at least 70% crystalline, or at least 80% crystalline, or at least 90% crystalline, or at least 95% crystalline, or at least 98% crystalline, or at least 99% crystalline, or at least 99.5% crystalline, or at least 99.9% crystalline, for example 100% crystalline.

The crystalline form of the compound of formula (1) is preferably one having a crystalline purity of at least 90%, more preferably at least 95%; i.e. at least 90% (more preferably at least 95%) of the compound is of a single crystalline form (e.g. Form A or Form B).

The crystalline forms of the compound of the invention may be solvated (e.g. hydrated) or non-solvated (e.g. anhydrous).

Patent covers control and manufacture of TYK2, A very small abstract.

'The TYK2 kinase-inhibiting activities of the crystalline forms of the compound of formula (1) can be made use of in various methods of treating diseases where TYK2 plays a part in the development or progression of the disease. The various uses of the compound of formula (1) typically involve bringing the compound into contact with a TYK2 kinase. The inhibition of the TYK2 kinase may take place either in vitro or in vivo.

Accordingly, in further embodiments, the invention provides:

6.1 A crystalline form of the compound of formula (1) as defined in any one of Embodiments 1.0 to 5.2 for use as an inhibitor of TYK2 kinase.

6.2 A crystalline forms of the compound of formula (1) as defined in any one of Embodiments 1.0 to 5.2 for use in medicine.

The inhibition of TYK2 kinase preferably takes place in vivo as part of a therapeutic treatment of a disease or condition in which TYK2 kinase is implicated.

The compound of formula (1) is a selective TYK2 inhibitor and is considerably more active against TYK2 than JAK2 and JAK3 kinases. The compound has relatively poor activity against a wide range of other kinases and, in particular, kinases that are generally recognised as targets for anti-cancer therapy. Thus, for example, the compounds have relatively little activity against Chk1 kinase, Aurora kinases, PKB (Akt) kinase and cyclin dependent kinases (CDK kinases) which are involved in cell cycle progression. A lack of activity against kinases typically considered to be anti-cancer targets is beneficial in compounds that may be used in chronic treatment of inflammatory and autoimmune diseases for example.

It is envisaged on the basis of their TYK2 inhibiting activity that the crystalline forms of the compound of formula (1) as defined in any one of Embodiments 1.0 to 5.2 will be useful in treating at least some of the diseases and disorders discussed below, including inflammatory diseases or conditions, immunological diseases or conditions, autoimmune diseases, allergic diseases or disorders, transplant rejections (allograft transplant rejections); Graft-versus host disease; treating sepsis and septic shock.

There exists hours of reading on the subject.

A great find who ever posted originally and a great post whoever subsequently reposted.

Regards

worth a read and apologies if posted before.

https://www.edisongroup.com/publication/treading-the-tyk2-trail/29435/

News due any time soon I feel.

Thanks for another good post with regards to jak 1 Citizen.

Jak1 is not all bad. it has side effects. Jaks work best in pairs and to a certain extent this is relied on. It becomes a matter of balance. Looking earlier at some of the older proactive interviews with Sareum with the smooth talking Aussie Andrew Scott. Tims ums and ahhs but also constantly looking at the safety side and tweaks to improve,

AS is one of the targets of 1801. I will look further into the implications of whether they can tweak a compound for individual targets or whether the targets can be covered with compounds they can select from 0, 1, or group 2 molecules or combinations thereof. Without necessitating the need to go through the trials for a new compound each time.

regards

Notalot and Salfordred keep yourselves positive.

As Tim used the term 'optimum amount' with regards to Jak1 in our Tyk2 Jak one compound .

Regards

As far as I know all was fine with FLT +3 it was as stated by an earlier poster a problem with solubility issues. This proved troublesome in establishing a MTD and the oral route. Similar treatments were used in early stages as a route for Covid 19.

Fine in the lab but no use on bigger scale. Hemce the manufacturing of in large concentrated quantities was and until resolved still is.

Regards

I don't know of any regulars on this board who have not offered their support.

Regards

Not easy to achieve with some elements. However a basic outline given below.

A crystalline structure is any structure of ions, molecules, or atoms that are held together in an ordered, three-dimensional arrangement. Crystalline structure is one of two types of structural ordering of atoms, the other being the amorphous structure. The key difference in the crystalline and amorphous structure is the ordering of the structure. Crystalline structure can be thought of as the highest level of order that can exist in a material, while an amorphous structure is irregular and lacks the repeating pattern of a crystal lattice.

Simply, the crystal structure can be thought of as a small box with atoms, molecules, or ions located in specific areas of the box. The atoms within this box represent the smallest group of repeating atoms in the entire molecule. That means each atom found in the small box continues to repeat on and on in the same connectivity throughout the entire compound. The general arrangement and order of the atoms in the structure are directly related to the natural properties of the crystal. The crystalline structure is unique and specific for each material. That is to say,

' there will be no other compound organized in exactly the same way as any other. Essentially, the crystalline structure is the 'identification marker' for the compound'

Not much room for generic copies here then.

Still perusing through your article Stoney and point worthy of note is Sareum funding formulation specialists.

Regards

Good morning Stoney40. The Chinese pharma took on FLT+3 for 50k for supposedly looking for the oral route. Not think this were the case. Why would a pharma who took this on not want their name disclosed.

As I see it,It also belongs to the same family of compounds as SDC1801 and SDC1802. The molecules are covered by the original patents (for FLT I believe 2013), patent but would hazard a guess that the molecules and more importantly the crystallisation process ( part of manufacturing) which make up the compounds ( are now protected further ) whether 1801, 1802 or FLT3.

Tim did state around 18 month ago that they would have to outsource ( but this would also be costly) . They had pooled all the resources into 1801 and 1802. Now we reach a stage where these compounds will need to be manufactured in much larger quantities.

Importance of patent here is paramount. Sareum must have known about crystallisation years back and would hazard a guess this may have been used to make up small amounts for laboratory use.

Regards. We will know in around 11 to 12 days time.

Regards

Salfordred. I hope and pray all will be well with you and your wife. As we get older we fall foul of the ailments that many of the modern treatments are aimed at. They improve all the time. Early diagnosis leads to early treatment and earlier recovery. I cam empathise with you. Keep your spirits up and am sure all will work out fine for you both.

Regards

One aspect of the patent protection is likely to be the manufacture of compounds. If the compounds can only be manufactured to an acceptable quality via this route then it will add vastly more protection and more importantly longer protection, with a corresponding higher net worth of the compounds covered by this newly patented invention.

Worked a blinder if this is the case,,as has already been mentioned.

My own worthless opinion is we will receive an RNS detailing patent 1700 hrs 26th October or 7.00 am 27th October. I cannot see duck bottom watertight or Camels bottom in a sandstorm tight Sareum letting the cat out of the bag before then.

Regards

Good read Citizen79. Jak1 and Tyk2 rules. Will get tee shirt made. Should go well with the Horseshoe Bats And Pangolins my ar5e.. IL-6 inhibition. Pure Tyk 2 no good, Jak2 mess selective. Jak 3 not compatible with Tyk 2 and of no use in production of IL-6 anyway.

Regards

Pie eyed. I have one tv in room, yet i can see two. I cannot focus fully on either.

What we see at times is not actually what we see but our perception of.

One more bootle of Henry Westons and SOG out for count.

Regards and good night all. Have faith and all will come to fruition. A waiting game and mothing elsse