Patent US4351844A successfully refreshed from Google Patents.
← Back to Patent Explorer
US4351844A Expired / Lapsed US ⏱️ 0.0 years remaining

Hypocholesterolemic hydrogenation products and process of preparation

Assignee: Merck and Co Inc
•
Filing: 1980-12-01
•
Granted: 1982-09-28
•
Expires: 2000-12-01
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract Hydrogenation of the natural fermentation product, mevinolin, MK-803, results in the production of dihydro- and tetra-hydro derivatives and hydrogenation of the naturally occurring dihydromevinolin results in the formation of a tetrahydro derivative. These several products with the exception of cis-(4 alpha beta , 8 alpha beta -)-tetrahydromevinolin are potent inhibitors of cholesterol biosynthesis.

Inventors

  • 👤 Arthur A. Patchett
  • 👤 Chan-Hwa Kuo

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 10:52
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 89 words
A compound of the formula: ##STR5## and its free acid form ##STR6## in which the dotted lines indicated as A and B represent optional double bonds, not more than one of A and B being a double bond, and, where neither A nor B is a double bond, the perhydronaphthyl ring is in the 4aα, 8aβ configuration, together with the pharmaceutically acceptable salts of said free acid and the lower alkyl and substituted lower alkyl esters of said free acid in which said substituent is phenyl, dimethylamino or acetylamino.
Claim 2
Dependent Claim 89 words
A compound of the formula: ##STR5## and its free acid form ##STR6## in which the dotted lines indicated as A and B represent optional double bonds, not more than one of A and B being a double bond, and, where neither A nor B is a double bond, the perhydronaphthyl ring is in the 4aα, 8aβ configuration, together with the pharmaceutically acceptable salts of said free acid and the lower alkyl and substituted lower alkyl esters of said free acid in which said substituent is phenyl, dimethylamino or acetylamino.
Claim 3
Dependent Claim 12 words
The compound of claim 1 which is the lactone of Formula II.
Claim 4
Dependent Claim 14 words
The pharmaceutically acceptable salts of the free acid of Formula III of claim 1.
Claim 5
Dependent Claim 8 words
The esters of Compound III of claim 1.
Claim 6
Dependent Claim 10 words
The free acid form of Compound III of claim 1.
Claim 7
Dependent Claim 12 words
The compounds of claim 2 in which A is a double bond.
Claim 8
Dependent Claim 12 words
The compound of claim 2 in which B is a double bond.
Claim 9
Dependent Claim 21 words
The compounds of claim 2 in which neither A nor B is a double bond and the ring system is transfused.
Claim 10
Dependent Claim 33 words
A method of treating hypercholesterolemia which comprises the administration to a patient in need of such treatment of an effective antihypercholesterolemic amount of a compound of formula II or III of claim 1.
Claim 11
Dependent Claim 24 words
An antihypercholesterolemic pharmaceutical composition comprising a pharmaceutical carrier and an antihypocholesterolemic effective amount of a compound of formula II or III of claim 1.

References Cited (Backward Citations)

US3072709A Cited
US3344169A Cited
US4293446A Cited
US4323648A Cited
US4231938A Cited
US4319039A Cited
US4294846A Cited
US4282155A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-09-27 1986-03-29 1986-09-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-09-27 1990-03-29 1990-09-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-09-27 1994-03-29 1994-09-28 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag