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Q: History of Pharmaceuticals ( No Answer,   2 Comments )
Subject: History of Pharmaceuticals
Category: Science > Chemistry
Asked by: scienceguy123-ga
List Price: $100.00
Posted: 15 Dec 2005 17:31 PST
Expires: 14 Jan 2006 17:31 PST
Question ID: 606353
In what year, and preferably what month, was the drug "lisinopril"
first synthesized (made)?

Lisinopril is a Angiotensin-Converting Enzyme (ACE) inhibitor used in
the treatment of high-blood pressure. Merck & Co., Inc. holds a patent
for the compound, which patent was applied for in the US on December
11, 1978 (note--that does NOT mean that it was first synthesized on
that date). Lisinopril is marketed in dozens of countries around the
world under in formulations under the names Prinovil and Zestril.

Request for Question Clarification by pafalafa-ga on 16 Dec 2005 03:54 PST
Can you identify the specific patent you have in mind (that was filed
on December 11, 1978)?

It would be helpful.


Clarification of Question by scienceguy123-ga on 16 Dec 2005 07:46 PST
The patent application was U.S. Ser. No. 968,249. Several
continuations-in-part (further applications) were filed after this
application. Ultimately, the patent issued as US Patent Number
4,374,829 on February 22, 1983. Lisinopril is claim 29 of that patent.
The listed inventors are Wyvratt, Harris, Patchett and Tristram.
There is no answer at this time.

Subject: Re: History of Pharmaceuticals
From: muham-ga on 16 Dec 2005 13:36 PST
This is a hard thing to answer unless you have an inside scoop -
something like a copy of the actual notebook or some other internal
company document.

The best you can do in this case as an outsider is to look up the
preceding patents on this class of compound - if lisinopril structure
is not there in the preceding patent, it is most likely that it was
not made at the time of filing of the preceding patent. But there are
continuations etc.

You should hire a patent expert to do the analysis for you - your
question is generic form availability, isn't it? To know when the
compound is off patent. You will probably have to pay more to get a
reliable info of this kind.

Btw., have you ever tried to contact Merck and ask them directly?
Maybe they will tell you.
Subject: Re: History of Pharmaceuticals
From: dr_bob-ga on 07 Jan 2006 15:51 PST
you can do a structure search on the compound and find when first
disclosure of it's structure was made (which may be different than its
disclosure as an ACE inhibitor).  when it was absolutely first
made.... you're better off to write the people in the first paper and
they'll tell you.

sometimes things sit on a benchtop for years before they get tested.

I agree, contact Merck, you might be surprised.  That information may
or may not be proprietary.


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