JP2002533336A5 - - Google Patents
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- Publication number
- JP2002533336A5 JP2002533336A5 JP2000589531A JP2000589531A JP2002533336A5 JP 2002533336 A5 JP2002533336 A5 JP 2002533336A5 JP 2000589531 A JP2000589531 A JP 2000589531A JP 2000589531 A JP2000589531 A JP 2000589531A JP 2002533336 A5 JP2002533336 A5 JP 2002533336A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- aryl
- cycloalkyl
- arylalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 description 82
- 125000000753 cycloalkyl group Chemical group 0.000 description 56
- 125000003710 aryl alkyl group Chemical group 0.000 description 54
- 125000003118 aryl group Chemical group 0.000 description 53
- 125000001424 substituent group Chemical group 0.000 description 36
- 150000001875 compounds Chemical class 0.000 description 34
- 229910052799 carbon Inorganic materials 0.000 description 28
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 28
- 210000004881 tumor cell Anatomy 0.000 description 25
- 125000005843 halogen group Chemical group 0.000 description 20
- 125000001072 heteroaryl group Chemical group 0.000 description 20
- 150000001721 carbon Chemical group 0.000 description 18
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 15
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 13
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 10
- 229910052757 nitrogen Inorganic materials 0.000 description 10
- -1 dihalo Chemical group 0.000 description 8
- 125000002883 imidazolyl group Chemical group 0.000 description 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 description 6
- 125000003107 substituted aryl group Chemical group 0.000 description 6
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 150000001408 amides Chemical group 0.000 description 5
- 229910052760 oxygen Inorganic materials 0.000 description 5
- 239000001301 oxygen Substances 0.000 description 5
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 4
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 0 *c1cnc(C2(CC2)C2C=CC(*)=CC2CC2)c2c1 Chemical compound *c1cnc(C2(CC2)C2C=CC(*)=CC2CC2)c2c1 0.000 description 3
- 206010005003 Bladder cancer Diseases 0.000 description 3
- 206010006187 Breast cancer Diseases 0.000 description 3
- 208000026310 Breast neoplasm Diseases 0.000 description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 3
- 102000004357 Transferases Human genes 0.000 description 3
- 108090000992 Transferases Proteins 0.000 description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 3
- 201000011510 cancer Diseases 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 208000029742 colonic neoplasm Diseases 0.000 description 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 3
- 125000004030 farnesyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])C([H])([H])C([H])=C(C([H])([H])[H])C([H])([H])C([H])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 201000005202 lung cancer Diseases 0.000 description 3
- 208000020816 lung neoplasm Diseases 0.000 description 3
- 201000001441 melanoma Diseases 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 210000000066 myeloid cell Anatomy 0.000 description 3
- 208000025113 myeloid leukemia Diseases 0.000 description 3
- 201000002528 pancreatic cancer Diseases 0.000 description 3
- 208000023958 prostate neoplasm Diseases 0.000 description 3
- 210000001685 thyroid gland Anatomy 0.000 description 3
- 201000005112 urinary bladder cancer Diseases 0.000 description 3
- 125000000304 alkynyl group Chemical group 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 125000004430 oxygen atom Chemical group O* 0.000 description 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 125000000547 substituted alkyl group Chemical group 0.000 description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
- ZBADMPXWYOLEJS-FLEGBKSUSA-N CC(C)OC(N(CC[N](C1)([C@@H](C(C=C2)=C(CC3)C(C)C2Cl)c(nc2)c3cc2Br)#C)[C@H]1C#CC(NCCC(C)(C)N1C#[N]CC1)=O)=O Chemical compound CC(C)OC(N(CC[N](C1)([C@@H](C(C=C2)=C(CC3)C(C)C2Cl)c(nc2)c3cc2Br)#C)[C@H]1C#CC(NCCC(C)(C)N1C#[N]CC1)=O)=O ZBADMPXWYOLEJS-FLEGBKSUSA-N 0.000 description 1
- 101150040459 RAS gene Proteins 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 108700042226 ras Genes Proteins 0.000 description 1
- 102000016914 ras Proteins Human genes 0.000 description 1
- 108010014186 ras Proteins Proteins 0.000 description 1
- 231100000588 tumorigenic Toxicity 0.000 description 1
- 230000000381 tumorigenic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21639898A | 1998-12-18 | 1998-12-18 | |
| US09/216,398 | 1998-12-18 | ||
| PCT/US1999/027939 WO2000037459A1 (en) | 1998-12-18 | 1999-12-16 | Tricyclic farnesyl protein transferase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002533336A JP2002533336A (ja) | 2002-10-08 |
| JP2002533336A5 true JP2002533336A5 (OSRAM) | 2007-02-08 |
Family
ID=22806914
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000589531A Pending JP2002533336A (ja) | 1998-12-18 | 1999-12-16 | 三環式ファルネシルタンパク質トランスフェラーゼインヒビター |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1140902A1 (OSRAM) |
| JP (1) | JP2002533336A (OSRAM) |
| KR (1) | KR20010081116A (OSRAM) |
| CN (1) | CN1326850C (OSRAM) |
| AR (1) | AR021718A1 (OSRAM) |
| AU (1) | AU776558B2 (OSRAM) |
| BR (1) | BR9916314A (OSRAM) |
| CA (1) | CA2354779A1 (OSRAM) |
| CO (1) | CO5160350A1 (OSRAM) |
| CZ (1) | CZ20011950A3 (OSRAM) |
| HU (1) | HUP0202152A2 (OSRAM) |
| IL (1) | IL143408A0 (OSRAM) |
| NO (1) | NO20012961L (OSRAM) |
| NZ (1) | NZ511878A (OSRAM) |
| PE (1) | PE20001342A1 (OSRAM) |
| PL (1) | PL348293A1 (OSRAM) |
| SK (1) | SK7592001A3 (OSRAM) |
| TR (1) | TR200101755T2 (OSRAM) |
| WO (1) | WO2000037459A1 (OSRAM) |
| ZA (1) | ZA200104233B (OSRAM) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR021718A1 (es) | 1998-12-18 | 2002-07-31 | Schering Corp | Inhibidores de transferasa de proteina farnesilo. |
| US7342016B2 (en) | 2000-08-30 | 2008-03-11 | Schering Corporation | Farnesyl protein transferase inhibitors as antitumor agents |
| AU2002236813A1 (en) * | 2001-01-22 | 2002-07-30 | Schering Corporation | Treatment of malaria with farnesyl protein transferase inhibitors |
| AU2002257114A1 (en) * | 2001-04-06 | 2002-10-21 | Schering Corporation | Treatment of malaria with farsenyl protein transferase inhibitors |
| US7585864B2 (en) | 2004-12-13 | 2009-09-08 | Schering Corporation | Farnesyl protein transferase inhibitors and their use to treat cancer |
| EP1833481A1 (en) | 2004-12-14 | 2007-09-19 | Schering Corporation | Farnesyl protein transferase inhibitors and methods for treating proliferative diseases |
| CA2637572A1 (en) * | 2006-01-19 | 2007-07-26 | Schering Corporation | Piperazine derivatives as farnesyl protein transferase inhibitors |
| JP6613391B2 (ja) * | 2014-03-19 | 2019-12-04 | ブイピーエス‐３，インコーポレイテッド | ２−（２，４−ジフルオロフェニル）−１，１−ジフルオロ−１−（５−置換ピリジン−２−イル）−３−（１ｈ−テトラゾール−１−イル）プロパン−２−オールおよびその調製工程 |
| CN109678791B (zh) | 2014-03-19 | 2022-07-01 | 美国陶氏益农公司 | 1-(2,4-二氟苯)-2,2-二氟-2-(5-取代吡啶-2-基)乙酮及制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111235A (en) * | 1993-10-15 | 2001-03-19 | Schering Plough Corp | Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them |
| US5712280A (en) | 1995-04-07 | 1998-01-27 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| IL117798A (en) | 1995-04-07 | 2001-11-25 | Schering Plough Corp | Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them |
| US5801175A (en) * | 1995-04-07 | 1998-09-01 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| PE92098A1 (es) * | 1996-07-31 | 1998-12-31 | Schering Corp | N-cianoiminas triciclicas utiles como inhibidores de transferasa de proteina farnesilo |
| KR100640672B1 (ko) | 1997-06-17 | 2006-11-02 | 파마코페이아 드럭 디스커버리, 인크. | 파르네실 단백질 트랜스퍼라제의 억제에 유용한 벤즈피리도 사이클로헵탄 화합물 및 이를 포함하는 약제학적 조성물 |
| AR021718A1 (es) | 1998-12-18 | 2002-07-31 | Schering Corp | Inhibidores de transferasa de proteina farnesilo. |
-
1999
- 1999-12-16 AR ARP990106461A patent/AR021718A1/es unknown
- 1999-12-16 SK SK759-2001A patent/SK7592001A3/sk unknown
- 1999-12-16 CN CNB99816206XA patent/CN1326850C/zh not_active Expired - Fee Related
- 1999-12-16 CZ CZ20011950A patent/CZ20011950A3/cs unknown
- 1999-12-16 BR BR9916314-4A patent/BR9916314A/pt not_active IP Right Cessation
- 1999-12-16 EP EP99963980A patent/EP1140902A1/en not_active Withdrawn
- 1999-12-16 WO PCT/US1999/027939 patent/WO2000037459A1/en not_active Ceased
- 1999-12-16 PL PL99348293A patent/PL348293A1/xx not_active Application Discontinuation
- 1999-12-16 TR TR2001/01755T patent/TR200101755T2/xx unknown
- 1999-12-16 JP JP2000589531A patent/JP2002533336A/ja active Pending
- 1999-12-16 CA CA002354779A patent/CA2354779A1/en not_active Abandoned
- 1999-12-16 HU HU0202152A patent/HUP0202152A2/hu unknown
- 1999-12-16 IL IL14340899A patent/IL143408A0/xx unknown
- 1999-12-16 AU AU20307/00A patent/AU776558B2/en not_active Ceased
- 1999-12-16 CO CO99078843A patent/CO5160350A1/es unknown
- 1999-12-16 NZ NZ511878A patent/NZ511878A/en unknown
- 1999-12-16 KR KR1020017007632A patent/KR20010081116A/ko not_active Abandoned
- 1999-12-17 PE PE1999001295A patent/PE20001342A1/es not_active Application Discontinuation
-
2001
- 2001-05-23 ZA ZA200104233A patent/ZA200104233B/en unknown
- 2001-06-15 NO NO20012961A patent/NO20012961L/no not_active Application Discontinuation
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