Heterocyclic inhibitors of farnesyl protein transferase.
Abstract
Inhibition of farnesyl protein transferase is effected by compounds of the formula its enantiomers, diastereomers, pharmaceutically acceptable salts, prodrugs or solvates thereof, wherein: A₁ and A₂ are each independently H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, phenyl or substituted phenyl; G₁ is S or O; G₂ is H, -C(O)OH, -C(O)NH₂, 5-tetrazolyl, -C(O)N(R₇)OH or -CH₂OH; X is O or R₈N; Y and Z are each independently -CH₂- or -C(O)-; R₁, R₂, R₃, R₄, R₅, R₆ and R₇ are each independently H or alkyl; R₁ may also be alkanoyl, R₁ and A₁ taken together may be -(CH₂)m; R₈ is H, alkyl, phenyl, phenylalkyl, substituted phenyl, (substituted phenyl)alkyl or -C(O)R₉; R₉ is H, alkyl, phenyl, phenylalkyl, substituted phenyl or (substituted phenyl)alkyl; m is 3 or 4; n is 0, 1 or 2; p is 0, 1 or 2; and q is 0 or 1, with the proviso that when p is 0, then q is also 0.

Term
Term ended
Projected expiry passed 29 March 2014, 12.5 years ago.
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- Projected expiry
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1 sheet
Sheet 1
Every citation, both ways
| Document | Relation | Office | Category | Cited during | Relevant claims |
|---|---|---|---|---|---|
| EP0456180A1 | Cites | European Patent Office (EPO) | A | Search report | 1-19 |
| EP0461869A2 | Cites | European Patent Office (EPO) | A | Search report | 1-19 |
| EP0523873A1 | Cites | European Patent Office (EPO) | A | Search report | 1-19 |
| EP0528486A2 | Cites | European Patent Office (EPO) | A | Search report | 1-19 |
19 members in 12 offices
Priority claims8
| Document | Office | Kind | Date |
|---|---|---|---|
| 42377 | United States of America | – | |
| 4237793 | United States of America | A | |
| 4237793 | United States of America | A | |
| 85338 | United States of America | – | |
| 8533893 | United States of America | A | |
| 8533893 | United States of America | A | |
| US19930042377 | – | – | – |
| US19930085338 | – | – | – |
Members19
| Document | Office | Kind | |
|---|---|---|---|
| NO941181D0 | Norway | D0 | |
| FI941519A0 | Finland | A0 | |
| IL108999A0 | Israel | A0 | |
| IL108999D0 | Israel | D0 | |
| HU9400946D0 | Hungary | D0 | |
| CA2118985A1 | Canada | A1 | |
| FI941519A | Finland | A | |
| NO941181L | Norway | L | |
| EP0618221A2 | European Patent Office (EPO) | A2 | |
| AU5918494A | Australia | A | |
| ZA941902B | South Africa | B | |
| CZ69094A3 | Czechia | A3 | |
| CN1098408A | China | A | |
| EP0618221A3This record | European Patent Office (EPO) | A3 | |
| JPH0789935A | Japan | A | |
| HUT68080A | Hungary | A | |
| NZ260137A | New Zealand | A | |
| AU679716B2 | Australia | B2 | |
| IL108999A | Israel | A |
12 legal events, as 2 offices reported them to INPADOC
Over the term
Point at a mark for the eventEvents
| Event | Code | Office | |
|---|---|---|---|
| Applications withdrawn, deemed to be withdrawn, or refused after publication in hong kongWithdrawnWD | WD | HK | |
| Application refused18R | 18R | EP | |
| Information on the status of an ep patent application or granted ep patentGrantedSTATUS: THE APPLICATION HAS BEEN REFUSEDSTAA | STAA | EP | |
| First examination report despatched17Q | 17Q | EP | |
| Despatch of communication of intention to grantORIGINAL CODE: EPIDOS AGRAGRAG | GRAG | EP | |
| Information provided on ipc code assigned before grant7C 07K 5/00 A, 7A 61K 38/00 BRIC1 | RIC1 | EP | |
| First examination report despatched17Q | 17Q | EP | |
| Request for examination filed17P | 17P | EP | |
| Designated contracting statesAK | AK | EP | |
| Search report despatchedORIGINAL CODE: 0009013PUAL | PUAL | EP | |
| Designated contracting statesAK | AK | EP | |
| Public reference made under article 153(3) epc to a published international application that has entered the european phaseORIGINAL CODE: 0009012PUAI | PUAI | EP |
Numbers
- Publication
- 0618221
- Publication, DOCDB
- 0618221
- Publication, EPODOC
- EP0618221
- Application
- 94302255
- Application, DOCDB
- 94302255
- Application, EPODOC
- EP19940302255
Titles3
- German
- Heterozyklische Farnesyl-Protein-Transferase-Inhibitoren
- English
- Heterocyclic inhibitors of farnesyl protein transferase
- French
- Inhibiteurs hétérocycliques de la farnesyl-protein-transferase
Classification
- CPC, 10
- C07K5/0821
- A61K38/00
- C07K5/06052
- C07K5/06139
- C07K5/0806
- C07K5/0808
- C07K5/0812
- C07K5/1013
- A61P35/00
- A61P43/00
- IPC, 25
- C12N9 99
- A61K31 40
- A61K31 403
- A61K31 404
- A61K31 47
- A61K31 472
- A61K38 00
- A61K38 05
- A61K38 06
- A61K38 07
- A61P35 00
- A61P43 00
- C07D209 42
- C07D217 26
- C07D403 06
- C07D405 06
- C07D409 06
- C07K5 06
- C07K5 062
- C07K5 065
- C07K5 078
- C07K5 083
- C07K5 087
- C07K5 097
- C07K5 103
Designated states1
- Contracting states, 1
- Sweden