ES2171736T3 - Derivados de 2-quinolona inhibidores de farnesil-transferasa. - Google Patents
Derivados de 2-quinolona inhibidores de farnesil-transferasa.Info
- Publication number
- ES2171736T3 ES2171736T3 ES96937249T ES96937249T ES2171736T3 ES 2171736 T3 ES2171736 T3 ES 2171736T3 ES 96937249 T ES96937249 T ES 96937249T ES 96937249 T ES96937249 T ES 96937249T ES 2171736 T3 ES2171736 T3 ES 2171736T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- alkyloxy
- amino
- hydroxy
- halo
- 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.)
- Expired - Lifetime
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 16
- 125000003545 alkoxy group Chemical group 0.000 abstract 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 150000002431 hydrogen Chemical class 0.000 abstract 6
- 125000001475 halogen functional group Chemical group 0.000 abstract 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 4
- -1 amino, hydroxycarbonyl Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 125000004951 trihalomethoxy group Chemical group 0.000 abstract 1
- 125000004953 trihalomethyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto de fórmula (I), una forma estereoisomérica del mismo, una sal de adición de ácido o de base del mismo farmacéuticamente aceptable; en la que la línea de puntos representa un enlace opcional; X esoxígeno o azufre; R 1 es hidrógeno, alquilo C12, Ar 1 , Ar 2 -alquilo C1-6, quinolinil-alquilo C1-6, piridil-alquilo C1-6, hidroxi -alquilo C1-6, alquiloxi (C1-6)-alquilo C1-6, monoó di(alquil C1-6)-amino-alquilo C1-6, aminoalquilo C1-6, o un radical de fórmula -Alk 1 -C(=O)-R 9 , -Alk 1 -S(O)-R 9 ó -Alk 1 -S(O)2-R 9 , en la que Alk 1 es alcanodiílo C1-6, R 9 es hidroxi, alquilo C1-6, alquiloxi C1-6, amino, alquilamino C1-8 o alquilamino C1-8 sustituido con alquiloxicarbonilo C1-6; R 2 y R 3 son cada uno independientemente hidrógeno, hidroxi, halo, ciano, alquilo C1-6, alquiloxi C1-6, hidroxi-alquiloxi C1-6, alquiloxi (C1-6)-alquiloxi C1-6, amino-alquiloxi C1-6, monoó di(alquil C1-6)-amino -alquiloxi C1-6, Ar 1 , Ar 2 -alquilo C1-6, Ar 2 -oxi, Ar 2 -alquiloxi C1-6, hidroxicarbonilo, alcoxicarbonilo C1-6, trihalometilo, trihalometoxi, alquenilo C2-6; ó cuando en posiciones contiguas R 2 y R 3 tomados conjuntamente pueden formar un radical bivalente de fórmula -O-CH2-O(a-1), -O-CH2-CH2-O(a-2), -O-CH=CH(a-3), -O-CH2-CH2(a-4), -O-CH2-CH2-CH2(a-5), ó -CH=CH-CH=CH(a-6); R 4 y R 5 son cada uno independientemente hidrógeno, Ar 1 , alquilo C1-6, alquiloxi (C1-6) alquilo C1-6, alquiloxi C1-6, alquiltio C1-6, amino, hidroxicarbonilo, alquiloxicarbonilo C1-6, alquil(C1-6) S(O) alquilo C1-6 ó alquil(C1-6) -S(O)2 alquilo C1-6; R 6 y R 7 son cada uno independientemente hidrógeno, halo, ciano, alquilo C1-6, alquiloxi C1-6 ó Ar 2 oxi; R 8 es hidrógeno, alquilo C1-6, ciano, hidroxicarbonilo, alquiloxicarbonilo C1-6, alquilcarbonil (C1-6) alquilo C1-6, ciano alquilo C1-6, alquiloxicarbonil (C1-6) alquilo C1-6, hidroxicarbonil alquilo C1-6, hidroxi alquilo C1-6, amino alquilo C1-6, mono-ó di(alquil C1-6) amino alquilo C1-6, halo alquilo C1-6, alquiloxi (C1-6) alquilo C1-6, aminocarbonil alquilo C1-6, Ar 1 , Ar 2 alquiloxi (C1-6) alquilo C1-6, alquiltio (C1-6) alquilo C1-6; R 10 es hidrógeno, alquilo C1-6, alquiloxi C1-6 o halo; R 11 es hidrógeno o alquilo C1-6; Ar 1 es fenilo o fenilo sustituido con alquilo C1-6, hidroxi, amino, alquiloxi C1-6 o halo; y Ar 2 es fenilo o fenilo sustituido con alquilo C1-6, hidroxi, amino, alquiloxi C1-6 ó halo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP95202945 | 1995-10-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2171736T3 true ES2171736T3 (es) | 2002-09-16 |
Family
ID=8220785
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES96937249T Expired - Lifetime ES2171736T3 (es) | 1995-10-31 | 1996-10-25 | Derivados de 2-quinolona inhibidores de farnesil-transferasa. |
| ES01200450T Expired - Lifetime ES2233557T3 (es) | 1995-10-31 | 1996-10-25 | Derivados de 2-quinolona que inhiben la farnesil transferasa. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES01200450T Expired - Lifetime ES2233557T3 (es) | 1995-10-31 | 1996-10-25 | Derivados de 2-quinolona que inhiben la farnesil transferasa. |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US5968952A (es) |
| EP (2) | EP1019395B1 (es) |
| JP (1) | JP4257869B2 (es) |
| KR (1) | KR100417620B1 (es) |
| CN (1) | CN1101391C (es) |
| AR (1) | AR004699A1 (es) |
| AT (2) | ATE269322T1 (es) |
| AU (1) | AU712435B2 (es) |
| CA (1) | CA2231143C (es) |
| CY (1) | CY2287B1 (es) |
| CZ (1) | CZ290954B6 (es) |
| DE (2) | DE69632751T2 (es) |
| DK (1) | DK1019395T3 (es) |
| EA (1) | EA000719B1 (es) |
| ES (2) | ES2171736T3 (es) |
| HU (1) | HU224032B1 (es) |
| IL (1) | IL123567A (es) |
| MY (1) | MY116577A (es) |
| NO (1) | NO314037B1 (es) |
| NZ (1) | NZ321576A (es) |
| PL (1) | PL184168B1 (es) |
| PT (1) | PT1019395E (es) |
| SI (1) | SI1019395T1 (es) |
| SK (1) | SK282642B6 (es) |
| TR (1) | TR199800720T2 (es) |
| TW (1) | TW349948B (es) |
| WO (1) | WO1997016443A1 (es) |
| ZA (1) | ZA969087B (es) |
Families Citing this family (91)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU740603B2 (en) * | 1997-06-02 | 2001-11-08 | Janssen Pharmaceutica N.V. | (imidazol-5-yl)methyl-2-quinolinone derivatives as inhibitors of smooth muscle cell proliferation |
| US6110461A (en) | 1997-08-13 | 2000-08-29 | Oncolytics Biotech Inc. | Reovirus for the treatment of neoplasia |
| US6136307A (en) | 1997-08-13 | 2000-10-24 | Oncolytics Biotech Inc. | Reovirus for the treatment of cellular proliferative disorders |
| US6565831B1 (en) | 1999-02-24 | 2003-05-20 | Oncolytics Biotech Inc. | Methods for preventing reovirus recognition for the treatment of cellular proliferative disorders |
| DK1037880T3 (da) | 1997-12-11 | 2004-11-15 | Janssen Pharmaceutica Nv | Anilider som retinsyremimetika |
| DK1097150T3 (da) * | 1998-06-16 | 2004-07-26 | Sod Conseils Rech Applic | Imidazolylderivater |
| US6420555B1 (en) | 1998-06-16 | 2002-07-16 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Imidazolyl derivatives |
| HRP20000904A2 (en) | 1998-07-06 | 2001-12-31 | Janssen Pharmaceutica Nv | Farnesyl protein transferase inhibitors for treating arthropathies |
| 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 |
| FR2780892B1 (fr) * | 1998-07-08 | 2001-08-17 | Sod Conseils Rech Applic | Utilisation d'inhibiteurs de prenyltransferases pour preparer un medicament destine a traiter les pathologies qui resultent de la fixation membranaire de la proteine g heterotrimerique |
| ID27562A (id) | 1998-08-27 | 2001-04-12 | Pfizer Prod Inc | Turunan-turunan kinolin-2-ona tersubstitusi alkunil yang berguna sebagai zat anti kanker |
| ES2237125T3 (es) | 1998-08-27 | 2005-07-16 | Pfizer Products Inc. | Derivados de quinolin-2-ona utiles como agentes anticancerigenos. |
| WO2000034239A2 (en) | 1998-12-08 | 2000-06-15 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| WO2000034437A2 (en) | 1998-12-08 | 2000-06-15 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| ID29241A (id) * | 1998-12-23 | 2001-08-16 | Janssen Pharmaceutica Nv | Turunan-turunan kinolin teranelasi-1,2 |
| PL349839A1 (en) | 1999-02-11 | 2002-09-23 | Pfizer Prod Inc | Heteroaryl-substituted quinolin-2-one derivatives useful as anticancer agents |
| US6143766A (en) * | 1999-04-16 | 2000-11-07 | Warner-Lambert Company | Benzopyranone and quinolone inhibitors of ras farnesyl transferase |
| EP1420015A1 (en) * | 1999-06-11 | 2004-05-19 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. | Imidazolyl derivatives |
| PT1106612E (pt) | 1999-11-30 | 2004-06-30 | Pfizer Prod Inc | Derivados de quinolina uteis para inibir a farnesil-proteina-transferase |
| HN2000000266A (es) * | 2000-01-21 | 2001-05-21 | Pfizer Prod Inc | Compuesto anticanceroso y metodo de separacion de enantiomeros util para sintetizar dicho compuesto. |
| US6838467B2 (en) | 2000-02-24 | 2005-01-04 | Janssen Pharmaceutica N. V. | Dosing regimen |
| JP2003525252A (ja) * | 2000-02-29 | 2003-08-26 | 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 | Ｈｅｒ２抗体とのファルネシルタンパク質トランスフェラーゼ阻害剤組み合わせ剤 |
| CA2397448A1 (en) * | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with further anti-cancer agents |
| US20030078281A1 (en) * | 2000-02-29 | 2003-04-24 | Rybak Mary Ellen Margaret | Farnesyl protein transferase inhibitor combinations with anti-tumor alkylating agents |
| US20030027808A1 (en) * | 2000-02-29 | 2003-02-06 | Palmer Peter Albert | Farnesyl protein transferase inhibitor combinations with platinum compounds |
| WO2001064196A2 (en) * | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with vinca alkaloids |
| EP1261343A2 (en) * | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with anti-tumor nucleoside derivatives |
| AU2001244167A1 (en) * | 2000-02-29 | 2001-09-12 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with anti-tumor anthracycline derivatives |
| AU2001252147A1 (en) * | 2000-02-29 | 2001-09-12 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations |
| WO2001064194A2 (en) * | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with camptothecin compounds |
| EP1267871A2 (en) * | 2000-02-29 | 2003-01-02 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with anti-tumor podophyllotoxin derivatives |
| JP2003525239A (ja) * | 2000-02-29 | 2003-08-26 | 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 | タキサン化合物とのファルネシルタンパク質トランスフェラーゼ阻害剤の組み合わせ剤 |
| US6844357B2 (en) * | 2000-05-01 | 2005-01-18 | Pfizer Inc. | Substituted quinolin-2-one derivatives useful as antiproliferative agents |
| JO2361B1 (en) * | 2000-06-22 | 2006-12-12 | جانسين فارماسيوتيكا ان. في | Enaniumer 1,2-anylated quinoline inhibitor for the transporter - farnesyl |
| US7067531B2 (en) * | 2000-09-25 | 2006-06-27 | Angibaud Patrick Rene | Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives |
| US7173040B2 (en) * | 2000-09-25 | 2007-02-06 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 6-[(substituted phenyl)methyl]-quinoline and quinazoline derinazoline derivatives |
| WO2002024682A1 (en) * | 2000-09-25 | 2002-03-28 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors |
| JP4348080B2 (ja) * | 2000-11-21 | 2009-10-21 | 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 | ファルネシルトランスフェラーゼを阻害するベンゾ複素環誘導体 |
| DK1339407T3 (da) * | 2000-11-28 | 2006-08-14 | Janssen Pharmaceutica Nv | Farnesylproteintransferaseinhibitorer til behandling af inflammatorisk tarmsygdom |
| CA2432137C (en) | 2000-12-19 | 2010-12-21 | Pfizer Products Inc. | Crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3h-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1h-quinolin-2-one, 2,3-dihydroxybutanedioate salts and method of production |
| ES2260316T3 (es) * | 2000-12-27 | 2006-11-01 | Janssen Pharmaceutica N.V. | Derivados de quinazolina y quinolina 4-sustituidos que inhiben la farnesil transferasa. |
| JP4351444B2 (ja) * | 2000-12-27 | 2009-10-28 | 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 | ファルネシルトランスフェラーゼを阻害する４−ヘテロシクリル−キノリンおよびキナゾリン誘導体 |
| 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 |
| BRPI0208075B8 (pt) | 2001-03-12 | 2021-05-25 | Janssen Pharmaceutica Nv | processo para a preparação de compostos de imidazol |
| US6740757B2 (en) | 2001-08-29 | 2004-05-25 | Pfizer Inc | Enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3h-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1h-quinolin-2-one and salts thereof, useful in the treatment of cancer |
| ATE425978T1 (de) | 2001-12-19 | 2009-04-15 | Janssen Pharmaceutica Nv | Durch c-verbundene imidazole substituierte 1,8- annellierten chinolon-derivate als farnesyl transferase inhibitoren |
| JP4450628B2 (ja) * | 2002-03-22 | 2010-04-14 | 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 | ファルネシルトランスフェラーゼインヒビターとして使用するためのベンジルイミダゾリル置換２−キノリンおよびキナゾリン誘導体 |
| ATE336496T1 (de) | 2002-04-15 | 2006-09-15 | Janssen Pharmaceutica Nv | Farnesyl transferase hemmende tricyclische quinazolinederivate substitutiert mit kohlenstoff-gebundenen imidazolen oder triazolen |
| FR2841243B1 (fr) * | 2002-06-19 | 2004-08-20 | Servier Lab | Nouveaux derives de 3-(4-oxo-4h-chromen-2yl)-(1h)-quinolein- 4-ones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US20030125268A1 (en) * | 2002-08-28 | 2003-07-03 | Rybak Mary Ellen Margaret | Farnesyl protein transferase inhibitor combinations with anti-tumor anthracycline derivatives |
| FR2860235A1 (fr) * | 2003-09-29 | 2005-04-01 | Yang Ji Chemical Company Ltd | Utilisation d'un compose de formule (i) inhibiteur de l'aromatase a des fins therapeutiques et composes de formule (i) en tant que tels |
| US20050272068A1 (en) * | 2004-03-18 | 2005-12-08 | The Brigham And Women's Hospital, Inc. | UCH-L1 expression and cancer therapy |
| CA2580767A1 (en) * | 2004-09-17 | 2006-03-30 | Whitehead Institute For Biomedical Research | Compounds, compositions and methods of inhibiting alpha-synuclein toxicity |
| HRP20130399T1 (hr) | 2004-11-05 | 2013-06-30 | Janssen Pharmaceutica Nv | Terapeutska upotreba inhibitora farenziltransferaze i postupci praä†enja njihove efikasnosti |
| US20060194821A1 (en) * | 2005-02-18 | 2006-08-31 | The Brigham And Women's Hospital, Inc. | Compounds inhibiting the aggregation of superoxide dismutase-1 |
| US20060281788A1 (en) * | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor |
| US20060281769A1 (en) * | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using thienopyrimidine and thienopyridine kinase modulators |
| US20060281755A1 (en) * | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using aminopyrimidines kinase modulators |
| US20070004660A1 (en) * | 2005-06-10 | 2007-01-04 | Baumann Christian A | Synergistic Modulation of Flt3 Kinase Using Alkylquinolines and Alkylquinazolines |
| US7833339B2 (en) | 2006-04-18 | 2010-11-16 | Franklin Industrial Minerals | Mineral filler composition |
| CA2634598A1 (en) | 2005-12-23 | 2007-07-05 | Link Medicine Corporation | Treatment of synucleinopathies |
| PL2021335T3 (pl) | 2006-04-20 | 2011-10-31 | Janssen Pharmaceutica Nv | Związki heterocykliczne jako inhibitory kinazy C-FMS |
| WO2007124319A1 (en) | 2006-04-20 | 2007-11-01 | Janssen Pharmaceutica N.V. | Inhibitors of c-fms kinase |
| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| DE102007015709B4 (de) | 2007-01-25 | 2009-09-03 | Webasto Ag | Fahrzeugdach |
| MY148609A (en) | 2007-06-05 | 2013-05-15 | Merck Sharp & Dohme | Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer |
| JO3240B1 (ar) | 2007-10-17 | 2018-03-08 | Janssen Pharmaceutica Nv | c-fms مثبطات كيناز |
| US7932036B1 (en) | 2008-03-12 | 2011-04-26 | Veridex, Llc | Methods of determining acute myeloid leukemia response to treatment with farnesyltransferase |
| WO2009151683A2 (en) * | 2008-03-12 | 2009-12-17 | Link Medicine Corporation | Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications |
| WO2009117484A2 (en) * | 2008-03-18 | 2009-09-24 | University Of South Florida | Small molecule e2f inhibitor |
| NZ593090A (en) | 2008-11-13 | 2013-06-28 | Link Medicine Corp | Azaquinolinone derivatives and uses thereof |
| JP2013506669A (ja) | 2009-09-30 | 2013-02-28 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｅｒｋ阻害剤である新規化合物 |
| WO2011127192A2 (en) | 2010-04-06 | 2011-10-13 | Brigham Young University | Antimetastatic compounds |
| WO2011163330A1 (en) | 2010-06-24 | 2011-12-29 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| ES2705719T3 (es) | 2010-07-28 | 2019-03-26 | Janssen Diagnostics Llc | Métodos de determinación de la respuesta de la leucemia mieloide aguda al tratamiento con inhibidores de la farnesiltransferasa |
| US20130158035A1 (en) * | 2010-08-24 | 2013-06-20 | Brigham Young University | Antimetastatic compounds |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| CN103906751A (zh) * | 2011-10-02 | 2014-07-02 | 波士顿大学董事会 | 作为晚期SV40因子（LSF）抑制剂用于治疗癌症的[1,3]二氧杂环戊烯并[4,5-g]喹啉-6(5H)-硫酮和[1,3]二氧杂环戊烯并[4,5-g][1,2,4]三唑并[1,5-a]喹啉衍生物 |
| CN104870454B (zh) | 2012-08-07 | 2020-03-03 | 詹森药业有限公司 | 用于制备杂环酯衍生物的方法 |
| ES2658773T3 (es) | 2012-08-07 | 2018-03-12 | Janssen Pharmaceutica N.V. | Procedimiento de sulfonilación usando fluoruro de nonafluorobutanosulfonilo |
| US10653672B2 (en) | 2014-02-07 | 2020-05-19 | National University Corporation Tokyo Medical And Dental University | Myogenesis promotor, muscle atrophy inhibitor, medical composition and TAZ activator |
| SMT202100712T1 (it) | 2015-08-17 | 2022-01-10 | Kura Oncology Inc | Metodi di trattamento di pazienti di cancro con inibitori di farnesil trasferasi |
| EP3133065A1 (en) | 2015-08-21 | 2017-02-22 | Merck Patent GmbH | Compounds for optically active devices |
| EP3133066A1 (en) * | 2015-08-21 | 2017-02-22 | Merck Patent GmbH | Hydrophilic compounds for optically active devices |
| US9815790B2 (en) | 2015-08-27 | 2017-11-14 | Janssen Pharmaceutica Nv | Chemically modified quinoline and quinolone derivatives useful as CB-1 inverse agonists |
| 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 |
| EP3363786A1 (en) | 2017-02-15 | 2018-08-22 | Merck Patent GmbH | Compounds for optically active devices |
| EP3363793A1 (en) | 2017-02-15 | 2018-08-22 | Merck Patent GmbH | Hydrophobic compounds for optically active devices |
| WO2019113269A1 (en) | 2017-12-08 | 2019-06-13 | Kura Oncology, Inc. | Methods of treating cancer patients with farnesyltransferase inhibitors |
| US20220143006A1 (en) | 2019-03-15 | 2022-05-12 | Kura Oncology, Inc. | Methods of treating cancer with farnesyltransferase inhibitors |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3900501A (en) * | 1970-12-23 | 1975-08-19 | Hoffmann La Roche | Benzophenone intermediates for 7-lower alkanoyl benzodiazepines |
| IL65709A (en) * | 1981-05-18 | 1986-01-31 | Chevron Res | Electroactive polymers |
| JPS63275548A (ja) * | 1987-05-02 | 1988-11-14 | Res Inst For Prod Dev | ｏ−アミノベンゾイル化合物の製造方法 |
| CA2002859C (en) * | 1988-11-29 | 1998-12-29 | Jean P. F. Van Wauwe | Method of treating epithelial disorders |
| CA2002864C (en) * | 1988-11-29 | 1999-11-16 | Eddy J. E. Freyne | (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives |
| EP0574992A1 (en) * | 1992-06-17 | 1993-12-22 | Glaxo Group Limited | 5-(1,2,4-Triazol-1-ylmethyl)-3H-isobenzofuran-1-one derivatives, their preparation and use as aromatase inhibitors |
| ES2134971T3 (es) * | 1994-04-15 | 1999-10-16 | Takeda Chemical Industries Ltd | Derivado de acido octahidro-2-naftaleno-carboxilico, su produccion y uso. |
-
1996
- 1996-10-24 TW TW085113018A patent/TW349948B/zh active
- 1996-10-25 PL PL96328230A patent/PL184168B1/pl unknown
- 1996-10-25 CA CA002231143A patent/CA2231143C/en not_active Expired - Lifetime
- 1996-10-25 EP EP96937249A patent/EP1019395B1/en not_active Expired - Lifetime
- 1996-10-25 IL IL12356796A patent/IL123567A/en not_active IP Right Cessation
- 1996-10-25 WO PCT/EP1996/004661 patent/WO1997016443A1/en not_active Ceased
- 1996-10-25 SK SK556-98A patent/SK282642B6/sk unknown
- 1996-10-25 SI SI9630453T patent/SI1019395T1/xx unknown
- 1996-10-25 PT PT96937249T patent/PT1019395E/pt unknown
- 1996-10-25 US US09/066,441 patent/US5968952A/en not_active Expired - Lifetime
- 1996-10-25 EP EP01200450A patent/EP1106610B1/en not_active Expired - Lifetime
- 1996-10-25 ES ES96937249T patent/ES2171736T3/es not_active Expired - Lifetime
- 1996-10-25 DK DK96937249T patent/DK1019395T3/da active
- 1996-10-25 TR TR1998/00720T patent/TR199800720T2/xx unknown
- 1996-10-25 HU HU9802424A patent/HU224032B1/hu not_active IP Right Cessation
- 1996-10-25 JP JP51705197A patent/JP4257869B2/ja not_active Expired - Lifetime
- 1996-10-25 ES ES01200450T patent/ES2233557T3/es not_active Expired - Lifetime
- 1996-10-25 AT AT01200450T patent/ATE269322T1/de not_active IP Right Cessation
- 1996-10-25 AU AU74933/96A patent/AU712435B2/en not_active Expired
- 1996-10-25 KR KR10-1998-0702088A patent/KR100417620B1/ko not_active Expired - Fee Related
- 1996-10-25 AT AT96937249T patent/ATE212627T1/de not_active IP Right Cessation
- 1996-10-25 NZ NZ321576A patent/NZ321576A/xx unknown
- 1996-10-25 EA EA199800395A patent/EA000719B1/ru not_active IP Right Cessation
- 1996-10-25 CZ CZ19981272A patent/CZ290954B6/cs not_active IP Right Cessation
- 1996-10-25 DE DE69632751T patent/DE69632751T2/de not_active Expired - Lifetime
- 1996-10-25 DE DE69618999T patent/DE69618999T2/de not_active Expired - Lifetime
- 1996-10-25 CN CN96197917A patent/CN1101391C/zh not_active Expired - Lifetime
- 1996-10-28 AR ARP960104942A patent/AR004699A1/es active IP Right Grant
- 1996-10-29 ZA ZA9609087A patent/ZA969087B/xx unknown
- 1996-10-30 MY MYPI96004530A patent/MY116577A/en unknown
-
1998
- 1998-03-04 NO NO19980928A patent/NO314037B1/no unknown
-
2002
- 2002-07-15 CY CY0200044A patent/CY2287B1/xx unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2171736T3 (es) | Derivados de 2-quinolona inhibidores de farnesil-transferasa. | |
| AR001440A1 (es) | Nuevos taxoides, su preparación y composiciones farmacéuticas que los contienen. | |
| ES2132339T3 (es) | Derivados sulfonato y carbamato de los 3-aroilbenzo(beta)tiofenos. | |
| BR0114630A (pt) | Secretagogos de hormÈnio do crescimento | |
| DK0833619T3 (da) | Styret frigivelse af lægemidler indgivet ved sublingual eller bukkal administration | |
| UY27169A1 (es) | Derivados del ácido isoftálico como inhibidores de metalproteinasas de la matriz | |
| BRPI0111116B8 (pt) | imitadores de trombopoietina | |
| ES2133163T3 (es) | Esteres (o tioesteres) del acido n-acilsulfamico y esteres (o tioesteres) del acido n-sulfonilcarbamico como agentes hipercolesterolemicos. | |
| ES2176600T3 (es) | Derivado de la propiofenona y procedimientos para su preparacion. | |
| ES2192201T3 (es) | Compuestos de piranona utiles para el tratamiento de infecciones retrovirales. | |
| BR9811099A (pt) | Inibidores de urocinase | |
| MX9605613A (es) | Procedimiento para preparar formas anhidras e hidratadas de derivados de piperidina antihistaminica, polimorfos y pseudomorfos de los mismos. | |
| CY1108334T1 (el) | Υποκατασταθεισες δικετοπιπεραζινες ως ανταγωνιστες ωκυτοκινης | |
| NO931536L (no) | Fremgangsmaater og sammensetninger for undertrykkelse av allograftforkastelse hos pattedyr | |
| AR002041A1 (es) | Nuevos taxoides, procedimiento para prepararlos, los compuestos intermediarios de aplicacion con dicho procedimiento, procedimiento parapreparar dichos intermediarios y las composiciones farmaceuticas que contienen dichos taxoides. | |
| NO974035L (no) | En ny vekstfaktor og en genetisk sekvens som koder for denne | |
| ES2062455T3 (es) | Nuevos derivados de benzonaftiridina-1,8, su preparacion y las composiciones que les contienen. | |
| WO2003029406A3 (en) | USE OF HIF-1α VARIANTS TO ACCELERATE WOUND HEALING | |
| AR245451A1 (es) | Un metodo de obtener n-fosfonometilglicina purificada a partir de una solucion acuosa que contiene n-fosfonometilglicina y diversas impurezas. | |
| ES2187816T3 (es) | Procedimiento y agentes para el moldeado duradero de fibras de queratina. | |
| ATE295165T1 (de) | Mittel zur adjuvanten therapie von demenzen enthaltend alpha-liponsäure | |
| MX9701334A (es) | Metodos para inhibir la degeneracion de protesis oseas. | |
| DK1232183T3 (da) | Peptider, som har antiangiogen aktivitet | |
| BR0207434A (pt) | Uso de agentes de domiciliação acelerada de linfócitos para a fabricação de um medicamento para o tratamento de função retardada de enxertos | |
| ES2112670T3 (es) | Derivados de ciclodextrina y su utilizacion, particularmente en cosmetica. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
Ref document number: 1019395 Country of ref document: ES |