Patent US2536750A successfully refreshed from Google Patents.
EP0535730A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Inhibitors of farnesyl protein transferase
Assignee: Merck and Co Inc
•
Filing: 1992-09-23
•
Granted: —
•
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
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 14:32
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06034; A; A61; A61P; A61P35/00; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0808; A61K; A61K38/00
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
143 words
A compound which inhibits farnesyl - protein transferase of the formula: wherein: X or Y 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 and R³ are the side chains of naturally occurring amino acids, or in the alternative may be substituted or unsubstituted aliphatic, aromatic or heterocyclic 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; Z is O or S; and n is 0, 1, or 2; or the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
142 words
A compound which inhibits farnesyl-protein transferase of the formula: wherein: X or Y 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 and R³ are the side chains of naturally occurring amino acids, or in the alternative may be substituted or unsubstituted aliphatic, aromatic or heterocyclic groups, such as allyl, cyclohexyl, phenyl, pyridyl, imidazolyl or saturated chains of 2 to 8 carbon atoms, wherein the aliphatic substitutuents may also be substituted with an aromatic or heteroaromatic ring; Z is O or S; and n is 0, 1, or 2; or the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
36 words
A compound which inhibits farnesyl-protein transferase which is: N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-homoserine, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl-homoserine, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-homoserine lactone, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl-homoserine lactone, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl-homocysteine lactone, N-[2(S)-(2(R)-amino-3-mercaptopropylamino)-3(S)-methyl pentyl]isoleucyl-homoserine lactone, N-[N'-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl]-3(S)-amino-tetrahydropyran-2-one, N-[N'-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl]-3(S)-amino-tetrahydropyran-2-one, N-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl-homocysteine lactone, N-[2(S)-(2(R)-amino-3-mercaptopropylamino)-3(S)-methyl pentyl]isoleucyl-homoserine, N-[N'-(2(R)-amino-3-mercaptopropyl)isoleucyl-phenylalanyl]-3(S)-amino-4-hydroxypentanoic acid, or N-[N'-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl]-3(S)-amino-4-hydroxypentanoic acid, or the pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
15 words
A compound of Claim 1 which is: N-[2(S)-(2(R)-amino-3-mercaptopropylamino)-3(S)-methyl pentyl]isoleucyl-homoserine or the pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
16 words
A compound of Claim 1 which is: N-[2(S)-(2(R)-amino-3-mercaptopropylamino)-3(S)-methyl pentyl)isoleucyl-homoserine lactone or the pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
14 words
A compound of Claim 1 is: N-[N'-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl]-3(S)-amino-4-hydroxy-pentanoic acid or the pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
14 words
A compound of Claim 1 which is: N-[N'-(2(R)-amino-3-mercaptopropyl)isoleucyl-isoleucyl]-3(S)-aminotetrahydropyran-2-one or the pharmaceutically acceptable salts thereof.
Claim 8
Dependent Claim
22 words
A composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound according to Claims 1 through 7.
Claim 9
Dependent Claim
25 words
The use of a compound as claimed in claim 1 for the manufacture of a medicament for inhibiting farnesylation of Ras protein in a mammal.
Claim 10
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.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.