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 |
|---|---|---|---|
| EP00200373.9 | 2000-02-04 | ||
| EP00200373 | 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 |
| DE60230017D1 (de) * | 2001-02-15 | 2009-01-08 | Janssen Pharmaceutica Nv | Farnesyl-protein-transferase hemmer in kombination mit antiöstrogenen |
| WO2003047697A2 (en) * | 2001-11-30 | 2003-06-12 | Schering Corporation | Use of an farsenyl protein tranferase inhibitor in combination with other antineoplastic agents for the manufacture of a medicament against cancer |
| US7102251B2 (en) * | 2003-08-22 | 2006-09-05 | Distributed Power, Inc. | Bi-directional multi-port inverter with high frequency link transformer |
| JP2007510661A (ja) * | 2003-11-06 | 2007-04-26 | シェーリング コーポレイション | 乳癌の治療のための、ファルネシルトランスフェラーゼインヒビターと抗ホルモン剤との組合せ |
| RU2006124843A (ru) | 2003-12-12 | 2008-01-20 | Уайт (Us) | Хинолины, пригодные для лечения сердечно-сосудистого заболевания |
| 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 |
| CA2559282A1 (en) * | 2004-03-18 | 2005-09-29 | Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies |
| WO2005089518A2 (en) * | 2004-03-18 | 2005-09-29 | 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 |
| US20060194821A1 (en) * | 2005-02-18 | 2006-08-31 | The Brigham And Women's Hospital, Inc. | Compounds inhibiting the aggregation of superoxide dismutase-1 |
| EP1968591A4 (en) | 2005-12-23 | 2010-02-17 | Link Medicine Corp | 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 |
| JP2012508768A (ja) * | 2008-11-13 | 2012-04-12 | リンク・メディスン・コーポレーション | アザキノリノン誘導体及びその使用 |
| 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 |
| CA2888485C (en) | 2012-10-16 | 2021-01-26 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of ror.gamma.t |
| MY189505A (en) | 2012-10-16 | 2022-02-16 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of roryt |
| ES2619610T3 (es) | 2012-10-16 | 2017-06-26 | Janssen Pharmaceutica Nv | Moduladores de ROR-gamma-t de quinolinilo enlazado con heteroarilo |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| BR112016008215A2 (pt) | 2013-10-15 | 2017-09-26 | Janssen Pharmaceutica Nv | moduladores de quinolinila ligados por alquila de roryt |
| 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 |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| ES2742843T3 (es) | 2013-10-15 | 2020-02-17 | Janssen Pharmaceutica Nv | Moduladores de quinolinilo de ROR(gamma)t |
| HUE044698T2 (hu) | 2015-08-17 | 2019-11-28 | Kura Oncology Inc | Kezelési módszer rákos páciensek kezelésére farnezil-transzferáz inhibitorokkal |
| JP2019534290A (ja) | 2016-11-03 | 2019-11-28 | クラ オンコロジー， インコーポレイテッド | 癌の治療方法において使用するためのファルネシルトランスフェラーゼ阻害剤 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69620445T2 (de) * | 1995-12-08 | 2002-12-12 | Janssen Pharmaceutica N.V., Beerse | (imidazol-5-yl)methyl-2-chinolinoderivate als farnesyl protein transferase inhibitoren |
| 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 |
| WO2000001701A1 (en) * | 1998-07-02 | 2000-01-13 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| PL193464B1 (pl) * | 1998-07-06 | 2007-02-28 | Janssen Pharmaceutica Nv | Zastosowanie inhibitora białkowej transferazy farnezylowej |
| DE69923849T2 (de) * | 1998-08-27 | 2006-01-12 | Pfizer Products Inc., Groton | Quinolin-2-on-derivate verwendbar als antikrebsmittel |
| DK1140935T3 (da) * | 1998-12-23 | 2003-09-01 | Janssen Pharmaceutica Nv | 1,2-anellerede quinolinderivater |
| AU2292801A (en) * | 1999-12-22 | 2001-07-03 | Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The | Compositions and methods for treatment of breast cancer |
| ATE375794T1 (de) * | 2000-02-24 | 2007-11-15 | Janssen Pharmaceutica Nv | Dosierschema enthaldend farnesyl protein transferase inhibitoren für die behandlung von krebs |
| WO2001064252A2 (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 SI SI200130572T patent/SI1255537T1/sl unknown
- 2001-02-01 AU AU2001233726A patent/AU2001233726A1/en not_active Abandoned
- 2001-02-01 ES ES01905717T patent/ES2262626T3/es not_active Expired - Lifetime
- 2001-02-01 CA CA002396865A patent/CA2396865C/en not_active Expired - Lifetime
- 2001-02-01 WO PCT/EP2001/001032 patent/WO2001056552A2/en not_active Ceased
- 2001-02-01 DK DK01905717T patent/DK1255537T3/da active
- 2001-02-01 AT AT01905717T patent/ATE323474T1/de active
- 2001-02-01 PT PT01905717T patent/PT1255537E/pt unknown
- 2001-02-01 US US10/203,083 patent/US20030027839A1/en not_active Abandoned
- 2001-02-01 DE DE60118889T patent/DE60118889T2/de not_active Expired - Lifetime
- 2001-02-01 JP JP2001556244A patent/JP5491681B2/ja not_active Expired - Lifetime
- 2001-02-01 EP EP01905717A patent/EP1255537B1/en not_active Expired - Lifetime
-
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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