[extropy-chat] MitoKor- patent

Sat Dec 27 02:30:12 UTC 2003

The prospectus is 133 pages so have not read it all but i see 52 million
was spent pre-filing  may 2002, with over 20 million in reserve at that
time.

Given that the male 50% of the population have to rely on phytosterols,
isoflavones and not estrogens to compensate  and that the weak estrogens
, while relatively cheap (about 100$/month) are not gnerally accepted by
HMO's for anything beyond HRT it seems that a market would exist.

I see the logic that if 20-30 analogues each targeted to an orphan
preventive market must each go through the full cost of pre-market
development and  ramp-up costs it represents a formidable cost without a
proven market acceptance.

The add on functional groups might allow for novel All-In-One-Molecule
combinatorial chemistry.
In theory, for example ,  the piracetam molecule could make for  a
candidate as a "Linker Moiety L"

*********************************************
6,268,398.........

Briefly stated, the present invention is directed to the treatment of
mitochondria-associated diseases
by administration to a warm-blooded animal in need thereof an effective
amount of a compound having the following general structure (I):
##STR2##

where Ar is phenyl or naphthyl optionally substituted with 1 to 5
R.sub.2 groups and L is an optional linker moiety.

In one embodiment, Ar is phenyl, naphthyl, 4-bromonaphthyl,
3,5-di-t-butyl-4-hydroxyphenyl,
2-methoxy-4-carboxylphenyl, 2-chloro-4-carboxyl-5-methoxyphenyl
3,5-di-tetrafluoromethylphenyl, 3,5-difluorophenyl,
3,4,5-trimethoxyphenyl, 4-n-hexoxyphenyl,
4-fluorophenyl, 3-tri fluorophenyl, 2-carbinolphenyl,
2-chloro-5-methylphenyl, 3-carboxylphenyl,
3-carboxyl-4-hydroxyphenyl, 2-methyl-4-carboxylphenyl, 4-methoxyphenyl,
2-hydroxyphenyl,
4-(N-morphinol)phenyl, 3,4-dihydroxyphenyl, 2,4-dimethylphenyl,
2-methyl-4-hydroxyphenyl,
4-n-octylphenyl, 2-hydroxy-5-n-octylphenyl, 4-chlorophenyl, or
2-methyl-4-chlorophenyl.

In another embodiment the optional linker moiety L is not present, while
in a further embodiment L is
present and is --CH.sub.2 NH--, --CH.sub.2 CH.sub.2, --CH(OH)CH.sub.2
--, --CH.sub.2
N(CH.sub.3)-- or --NHC(.dbd.NH)--.

In still further embodiments, methods are disclosed for treating
mitochondria-associated diseases by
administering one or more compounds of structure (I) in the form of a
pharmaceutical composition.
Thus, pharmaceutical compositions are also disclosed comprising a
compound of structure (I) in
combination with a pharmaceutically acceptable carrier or diluent.

In the context of this invention, mitochondria-associated disease
include diseases in which free radical
mediated oxidative injury leads to tissue degeneration. diseases in
which cells inappropriately undergo
apoptosis, and diseases in which cells fail to undergo apoptosis. Thus.
the methods of this invention
include the treatment of a wide number of mitochondria-associated
diseases. including (but not
limited to Alzheimer's Disease, Parkinson's Disease, Huntington's
Disease, auto-immune disease,
diabetes mellitus (Type I or Type II), congenital muscular dystrophy,
fatal infantile myopathy,
"later-onset" myopathy, MELAS (mitochondrial encephalopathy, lactic
acidosis, and stroke), MIDD
(mitochondrial diabetes and deafness), MERFF (myoclonic epilepsy ragged
red fiber syndrome),
arthritis, NARP (Neuropathy; Ataxia; Retinitis Pigmentosa), MNGIE
(Myopathy and external
ophthalmoplegia; Neuropathy; Gastro-Intestinal; Encephalopathy), LNION
(Leber's; Hereditary;
Optic; Neuropathy), Kearns-Sayre disease, Pearson's Syndrome, PEO
(Progressive External
Ophthalmoplegia), Wolfram syndrome, DIDMOAD (Diabetes Insipidus,
Diabetes Mellitus, Optic
Atrophy, Deafness), Leigh's Syndrome, dystonia, schizophrenia, cancer
and psoriasis.
****************************************

Have not looked to see if or  how the intellectual property was
dispersed.
There seems to be at least 52 million of recapturable  IP possible.
The website is still up but there are no SEC filings aside from the IPO
withdrawal letter of May 2003.

History shows that very useful orphan compounds have been overlooked
before. Piracetam was an orphan since 1973 until an new analogue
levetiracetam began to roll out majorly after 2000.  Levamisole was an
orphan in 1970 and still is, in spite of analogues showing up in the
late 90's.
************************************

"Robert J. Bradbury" wrote:

> With regard to MitoKor.  They made a presentation at the AGE
> meeting in June 2002.  The evidence they presented
> suggested that estrogen (or its analogues) were effective
> antioxidants/free radical sinks within the mitochondria.
>
> This of course explains why in general women live longer
> than men.  Of course from a therapy standpoint the question
> becomes why should one pay $XXX for an estrogen related
> drug vs. $YYY (<< $XXX) for estrogen itself.
>
> The MitoKor executives were very up-front in their presentations
> that even though the felt they had compounds that were more
> effective than estrogen they felt the investment/drug approval
> climate made it pointless to attempt to pursue them.
>
> Robert
>
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