EP0535731A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Inhibitors of farnesyl protein transferase
Assignee: Merck and Co Inc
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Filing: 1992-09-23
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Granted: —
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Expires: 2012-09-23
Abstract
Abstract The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Inventors
- 👤 Samuel L. Graham
- 👤 S. Jane Desolms
- 👤 Victor M. Garsky
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 17:58
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0808; A; A61; A61P; A61P35/00; C07K5/02; C07K5/0207; C07K5/06; C07K5/06008; C07K5/06078; A61K; A61K38/00
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
152 words
A compound which inhibits farnesyl-protein transferase of the formula: wherein: X, Y and Z are independently H₂ or O, provided that at least one of these is H₂; R¹ is H, an alkyl group, an acyl group, an alkylsulfonyl group or arylsulfonyl group, wherein alkyl and acyl groups comprise straight chain or branched chain hydrocarbons of 1 to 6 carbon atoms, or in the alternative, R¹NH may be absent; R², R³ and R⁴ are the side chains of naturally occurring amino acids, or in the alternative may be substituted or unsubstituted aliphatic, aromatic or heteroaromatic groups, such as allyl, cyclohexyl, phenyl, pyridyl, imidazolyl or saturated chains of 2 to 8 carbon atoms, wherein the aliphatic substitutents may be substituted with an aromatic or heteroaromatic ring; R⁵ is H or a straight or branched chain aliphatic group, which may be substituted with an aromatic or heteroaromatic group; or the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
41 words
The compound of Claim 1, wherein the compound is: N-(3-phenyl-2(S)-(mercaptopropionylamino)prop-1-yl)isoleucyl-methionine, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-methionine, N-(3-mercaptopropyl)isoleucyl-phenylalanyl-methionine, N-(3-mercaptopropyl)valyl-isoleucyl-methionine, N-(2(R)-amino-3-mercaptopropyl)valyl-isoleucyl-methionine, N-(3-methyl-2(S)-(cysteinylamino)but-1-yl)phenylalanyl-methionine. N-(3-methyl-2(S)-(mercaptopropionylamino)but-1-yl)phenylalanyl-methionine, N-[2(S)-(2(R)-amino-3-mercaptopropylamino)-3(S)-methylpentyl]phenylalanyl-methionine, N-[2(S)-(3-mercaptopropylamino)-3(S)-methylpentyl] phenylalanyl-methionine, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-(methionine sulfone), N-(2(R)-amino-3-mercaptopropyl)isoleucyl-(p-iodo-phenylalanyl)-methionine, N-[2(R)-(cysteinyl-isoleucylamino)-3(S)-methylpentyl]methionine, N-[2(R)-(N'-(2(R)-amino-3-mercaptopropyl)-isoleucylamino)-3-phenyl-propyl]methionine, N-[2(R)-(N'-(2(R)-amino-3-mercaptopropyl)-isoleucylamino)-3(S)-methylpentyl]methionine, N-(3-mercaptopropyl)valyl-isoleucyl-methionine methyl ester, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-methionine ethyl ester, or N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-methionine benzyl ester or the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
14 words
The compound of Claim 1 which is: N-[2(S)-(2(R)-amino-3-mercaptopropylamino)-3(S)-methylpentyl]phenylalanyl-methionine or the pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
14 words
The compound of Claim 1 which is: N-(3-methyl-2(S)-(cysteinylamino)but-1-yl)phenylalanylmethionine or the pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
16 words
The compound of Claim 1 which is: N-2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-methionine ethyl ester or the pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
15 words
A composition comprising a pharmaceutical carrier, and a compound according to Claims 1 through 5.
Claim 7
Dependent Claim
22 words
The use of a compound as claimed in claim 1 for the manufacture of a medicament for inhibiting farnesylation of Ras protein.
Claim 8
Dependent Claim
19 words
The use of a compound as claimed in claim 1 for the manufacture of a medicament for treating cancer.
References Cited (Backward Citations)
No citation records indexed.
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