JP2003521509A5 - - Google Patents
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- Publication number
- JP2003521509A5 JP2003521509A5 JP2001556244A JP2001556244A JP2003521509A5 JP 2003521509 A5 JP2003521509 A5 JP 2003521509A5 JP 2001556244 A JP2001556244 A JP 2001556244A JP 2001556244 A JP2001556244 A JP 2001556244A JP 2003521509 A5 JP2003521509 A5 JP 2003521509A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkyloxy
- hydrogen
- amino
- hydroxy
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 description 238
- 125000003545 alkoxy group Chemical group 0.000 description 89
- 239000001257 hydrogen Substances 0.000 description 67
- 229910052739 hydrogen Inorganic materials 0.000 description 67
- 150000002431 hydrogen Chemical class 0.000 description 58
- 125000005843 halogen group Chemical group 0.000 description 39
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 39
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 37
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 description 24
- 125000003118 aryl group Chemical group 0.000 description 24
- -1 4,4-dimethyloxazolyl Chemical group 0.000 description 20
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 description 19
- 125000004093 cyano group Chemical group *C#N 0.000 description 19
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 16
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 description 15
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 13
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 8
- 239000002253 acid Substances 0.000 description 8
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 description 8
- 150000003839 salts Chemical class 0.000 description 8
- 125000004951 trihalomethoxy group Chemical group 0.000 description 8
- 125000004953 trihalomethyl group Chemical group 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 6
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 5
- 229910052760 oxygen Inorganic materials 0.000 description 5
- 239000001301 oxygen Substances 0.000 description 5
- 125000001424 substituent group Chemical group 0.000 description 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 4
- 125000003282 alkyl amino group Chemical group 0.000 description 4
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 description 4
- 125000004076 pyridyl group Chemical group 0.000 description 4
- 229910052717 sulfur Chemical group 0.000 description 4
- 239000011593 sulfur Chemical group 0.000 description 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 description 3
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 description 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 3
- 125000002883 imidazolyl group Chemical group 0.000 description 3
- PLHJCIYEEKOWNM-UHFFFAOYSA-N 6-[amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one Chemical compound CN1C=NC=C1C(N)(C=1C=C2C(C=3C=C(Cl)C=CC=3)=CC(=O)N(C)C2=CC=1)C1=CC=C(Cl)C=C1 PLHJCIYEEKOWNM-UHFFFAOYSA-N 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 2
- 125000004104 aryloxy group Chemical group 0.000 description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 2
- 125000001309 chloro group Chemical group Cl* 0.000 description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 2
- 125000001820 oxy group Chemical group [*:1]O[*:2] 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
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 2
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 description 1
- WOYOASASOHZEDR-UHFFFAOYSA-N 4-(3-chlorophenyl)-6-[(4-chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]-1-methylquinolin-2-one Chemical compound CN1C=NC=C1C(O)(C=1C=C2C(C=3C=C(Cl)C=CC=3)=CC(=O)N(C)C2=CC=1)C1=CC=C(Cl)C=C1 WOYOASASOHZEDR-UHFFFAOYSA-N 0.000 description 1
- ZMLMGCPNMBRTKN-UHFFFAOYSA-N 6-[(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-ethoxyphenyl)-1-methylquinolin-2-one;hydrate;hydrochloride Chemical compound O.Cl.CCOC1=CC=CC(C=2C3=CC(=CC=C3N(C)C(=O)C=2)C(C=2N(C=NC=2)C)C=2C=CC(Cl)=CC=2)=C1 ZMLMGCPNMBRTKN-UHFFFAOYSA-N 0.000 description 1
- QOFQBGVDXIFFKM-UHFFFAOYSA-N 6-[(4-chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]-4-(3-ethoxyphenyl)-1-methylquinolin-2-one Chemical compound CCOC1=CC=CC(C=2C3=CC(=CC=C3N(C)C(=O)C=2)C(O)(C=2N(C=NC=2)C)C=2C=CC(Cl)=CC=2)=C1 QOFQBGVDXIFFKM-UHFFFAOYSA-N 0.000 description 1
- ALKQAQOKGRWMSJ-UHFFFAOYSA-N 6-[amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-ethoxyphenyl)-1-methylquinolin-2-one Chemical compound CCOC1=CC=CC(C=2C3=CC(=CC=C3N(C)C(=O)C=2)C(N)(C=2N(C=NC=2)C)C=2C=CC(Cl)=CC=2)=C1 ALKQAQOKGRWMSJ-UHFFFAOYSA-N 0.000 description 1
- 125000004414 alkyl thio group Chemical group 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 125000005129 aryl carbonyl group Chemical group 0.000 description 1
- 125000005110 aryl thio group Chemical group 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 125000004997 halocarbonyl group Chemical group 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- QGZKDVFQNNGYKY-NJFSPNSNSA-N nitrogen-16 Chemical group [16NH3] QGZKDVFQNNGYKY-NJFSPNSNSA-N 0.000 description 1
- GQZSLPJPXSZYNE-UHFFFAOYSA-N quinazolin-7-ylmethanamine Chemical compound C1=NC=NC2=CC(CN)=CC=C21 GQZSLPJPXSZYNE-UHFFFAOYSA-N 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00200373 | 2000-02-04 | ||
| EP00200373.9 | 2000-02-04 | ||
| PCT/EP2001/001032 WO2001056552A2 (en) | 2000-02-04 | 2001-02-01 | Farnesyl protein transferase inhibitors for treating breast cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003521509A JP2003521509A (ja) | 2003-07-15 |
| JP2003521509A5 true JP2003521509A5 (https=) | 2009-06-18 |
| JP5491681B2 JP5491681B2 (ja) | 2014-05-14 |
Family
ID=8170976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001556244A Expired - Lifetime JP5491681B2 (ja) | 2000-02-04 | 2001-02-01 | 乳ガンの治療のためのファルネシルタンパク質トランスフェラーゼ阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US20030027839A1 (https=) |
| EP (1) | EP1255537B1 (https=) |
| JP (1) | JP5491681B2 (https=) |
| AT (1) | ATE323474T1 (https=) |
| AU (1) | AU2001233726A1 (https=) |
| CA (1) | CA2396865C (https=) |
| CY (1) | CY1105477T1 (https=) |
| DE (1) | DE60118889T2 (https=) |
| DK (1) | DK1255537T3 (https=) |
| ES (1) | ES2262626T3 (https=) |
| PT (1) | PT1255537E (https=) |
| SI (1) | SI1255537T1 (https=) |
| WO (1) | WO2001056552A2 (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7342016B2 (en) * | 2000-08-30 | 2008-03-11 | Schering Corporation | Farnesyl protein transferase inhibitors as antitumor agents |
| JP4969016B2 (ja) * | 2001-02-15 | 2012-07-04 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 抗エストロゲン剤とファルネシルプロテイントランスフェラーゼ阻害剤の組み合わせ物 |
| CN1617755A (zh) * | 2001-11-30 | 2005-05-18 | 先灵公司 | 法尼基蛋白转移酶抑制剂和其它抗肿瘤剂联合使用在制备抗癌症的药物中的应用 |
| US7102251B2 (en) * | 2003-08-22 | 2006-09-05 | Distributed Power, Inc. | Bi-directional multi-port inverter with high frequency link transformer |
| CA2544421A1 (en) * | 2003-11-06 | 2005-05-26 | Schering Corporation | Combination of a farnesyl transferase inhibitor with an antihormonal agent for the treatment of breast cancer |
| AU2004298486A1 (en) | 2003-12-12 | 2005-06-30 | Wyeth | Quinolines useful in treating cardiovascular disease |
| US20050272068A1 (en) * | 2004-03-18 | 2005-12-08 | The Brigham And Women's Hospital, Inc. | UCH-L1 expression and cancer therapy |
| CA2559285A1 (en) * | 2004-03-18 | 2005-09-29 | Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies |
| US20070293539A1 (en) * | 2004-03-18 | 2007-12-20 | Lansbury Peter T | Methods for the treatment of synucleinopathies |
| JP2007529555A (ja) * | 2004-03-18 | 2007-10-25 | ザ ブライハム アンド ウイメンズ ホスピタル， インコーポレイテッド | シヌクレイノパチーを治療する方法 |
| US20060106060A1 (en) * | 2004-03-18 | 2006-05-18 | The Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies (Lansbury) |
| US20050272722A1 (en) * | 2004-03-18 | 2005-12-08 | The Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies |
| US20060194821A1 (en) * | 2005-02-18 | 2006-08-31 | The Brigham And Women's Hospital, Inc. | Compounds inhibiting the aggregation of superoxide dismutase-1 |
| CA2634598A1 (en) | 2005-12-23 | 2007-07-05 | Link Medicine Corporation | Treatment of synucleinopathies |
| WO2009151683A2 (en) * | 2008-03-12 | 2009-12-17 | Link Medicine Corporation | Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications |
| US20110060005A1 (en) * | 2008-11-13 | 2011-03-10 | Link Medicine Corporation | Treatment of mitochondrial disorders using a farnesyl transferase inhibitor |
| US20100331363A1 (en) * | 2008-11-13 | 2010-12-30 | Link Medicine Corporation | Treatment of mitochondrial disorders using a farnesyl transferase inhibitor |
| NZ593090A (en) * | 2008-11-13 | 2013-06-28 | Link Medicine Corp | Azaquinolinone derivatives and uses thereof |
| EP2288195B1 (en) * | 2009-08-20 | 2019-10-23 | Samsung Electronics Co., Ltd. | Method and apparatus for operating a base station in a wireless communication system |
| US9290476B2 (en) | 2012-10-16 | 2016-03-22 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| CN105073729A (zh) | 2012-10-16 | 2015-11-18 | 詹森药业有限公司 | RORγt的苯基连接的喹啉基调节剂 |
| CN104884448A (zh) | 2012-10-16 | 2015-09-02 | 詹森药业有限公司 | Rorγt的杂芳基连接的喹啉基调节剂 |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| BR112016008258A2 (pt) | 2013-10-15 | 2017-10-10 | Janssen Pharmaceutica Nv | moduladores de ror?t de quinolinila |
| BR112016008215A2 (pt) | 2013-10-15 | 2017-09-26 | Janssen Pharmaceutica Nv | moduladores de quinolinila ligados por alquila de roryt |
| SMT202100712T1 (it) | 2015-08-17 | 2022-01-10 | Kura Oncology Inc | Metodi di trattamento di pazienti di cancro con inibitori di farnesil trasferasi |
| TW201818965A (zh) | 2016-11-03 | 2018-06-01 | 美商庫拉腫瘤技術股份有限公司 | 以法呢基轉移酶（ｆａｒｎｅｓｙｌ ｔｒａｎｓｆｅｒａｓｅ）抑制劑治療癌症病患之方法 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK283335B6 (sk) * | 1995-12-08 | 2003-06-03 | Janssen Pharmaceutica N. V. | (Imidazol-5-yl)metyl-2-chinolinónové deriváty, spôsob a medziprodukty na ich prípravu, ich použitie a farmaceutické kompozície na ich báze |
| US5874442A (en) * | 1995-12-22 | 1999-02-23 | Schering-Plough Corporation | Tricyclic amides useful for inhibition of G-protein function and for treatment of proliferative disease |
| US5994364A (en) * | 1996-09-13 | 1999-11-30 | Schering Corporation | Tricyclic antitumor farnesyl protein transferase inhibitors |
| TW591030B (en) * | 1997-03-10 | 2004-06-11 | Janssen Pharmaceutica Nv | Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles |
| RU2205831C2 (ru) * | 1997-04-25 | 2003-06-10 | Янссен Фармацевтика Н.В. | Хиназолиноны, ингибирующие фарнезилтрансферазу |
| US5925639A (en) * | 1997-06-17 | 1999-07-20 | Schering Corporation | Keto amide derivatives useful as farnesyl protein transferase inhibitors |
| US5852034A (en) * | 1997-06-17 | 1998-12-22 | Schering Corporation | Benzo(5,6)cycloheptapyridine cyclic ureas and lactams useful as farnesyl protein transferase inhibitors |
| US6096757A (en) * | 1998-12-21 | 2000-08-01 | Schering Corporation | Method for treating proliferative diseases |
| JP2002519427A (ja) * | 1998-07-02 | 2002-07-02 | メルク エンド カムパニー インコーポレーテッド | プレニル蛋白トランスフェラーゼ阻害薬 |
| ID26987A (id) * | 1998-07-06 | 2001-02-22 | Janssen Pharmaceutica Nv | Inhibitor-inhibitor transferase protein farnesil dengan sifat-sifat peka terhadap sinar radiasi in vivo |
| ES2237125T3 (es) * | 1998-08-27 | 2005-07-16 | Pfizer Products Inc. | Derivados de quinolin-2-ona utiles como agentes anticancerigenos. |
| ID29241A (id) * | 1998-12-23 | 2001-08-16 | Janssen Pharmaceutica Nv | Turunan-turunan kinolin teranelasi-1,2 |
| WO2001045740A2 (en) * | 1999-12-22 | 2001-06-28 | The Government Of The United States, Department Of Health And Human Services | Compositions and methods for treatment of breast cancer |
| US6838467B2 (en) * | 2000-02-24 | 2005-01-04 | Janssen Pharmaceutica N. V. | Dosing regimen |
| CA2397448A1 (en) * | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with further anti-cancer agents |
| US20020022633A1 (en) * | 2000-06-30 | 2002-02-21 | Williams Theresa M. | Inhibitors of prenyl-protein transferase |
-
2001
- 2001-02-01 JP JP2001556244A patent/JP5491681B2/ja not_active Expired - Lifetime
- 2001-02-01 CA CA002396865A patent/CA2396865C/en not_active Expired - Lifetime
- 2001-02-01 EP EP01905717A patent/EP1255537B1/en not_active Expired - Lifetime
- 2001-02-01 WO PCT/EP2001/001032 patent/WO2001056552A2/en not_active Ceased
- 2001-02-01 DE DE60118889T patent/DE60118889T2/de not_active Expired - Lifetime
- 2001-02-01 SI SI200130572T patent/SI1255537T1/sl unknown
- 2001-02-01 US US10/203,083 patent/US20030027839A1/en not_active Abandoned
- 2001-02-01 AU AU2001233726A patent/AU2001233726A1/en not_active Abandoned
- 2001-02-01 PT PT01905717T patent/PT1255537E/pt unknown
- 2001-02-01 ES ES01905717T patent/ES2262626T3/es not_active Expired - Lifetime
- 2001-02-01 AT AT01905717T patent/ATE323474T1/de active
- 2001-02-01 DK DK01905717T patent/DK1255537T3/da active
-
2004
- 2004-04-06 US US10/818,767 patent/US20040192726A1/en not_active Abandoned
-
2006
- 2006-07-18 CY CY20061100995T patent/CY1105477T1/el unknown
-
2008
- 2008-09-16 US US12/211,705 patent/US20090018164A1/en not_active Abandoned
-
2011
- 2011-01-06 US US12/985,579 patent/US20110098318A1/en not_active Abandoned
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