PE20000986A1 - Derivados de quinolin-2-ona alquinilsustituidos utiles como agentes anticancerosos - Google Patents
Derivados de quinolin-2-ona alquinilsustituidos utiles como agentes anticancerososInfo
- Publication number
- PE20000986A1 PE20000986A1 PE1999000862A PE00086299A PE20000986A1 PE 20000986 A1 PE20000986 A1 PE 20000986A1 PE 1999000862 A PE1999000862 A PE 1999000862A PE 00086299 A PE00086299 A PE 00086299A PE 20000986 A1 PE20000986 A1 PE 20000986A1
- Authority
- PE
- Peru
- Prior art keywords
- cr13r14
- alkyl
- ona
- quinolin
- cyane
- Prior art date
Links
- 239000002246 antineoplastic agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- -1 IMIDAZOLYL Chemical class 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 101100212791 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) YBL068W-A gene Proteins 0.000 abstract 1
- 102000004357 Transferases Human genes 0.000 abstract 1
- 108090000992 Transferases Proteins 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 229940100198 alkylating agent Drugs 0.000 abstract 1
- 239000002168 alkylating agent Substances 0.000 abstract 1
- 239000003242 anti bacterial agent Substances 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 229940088710 antibiotic agent Drugs 0.000 abstract 1
- 229940100197 antimetabolite Drugs 0.000 abstract 1
- 239000002256 antimetabolite Substances 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- GEAXLHPORCRESC-UHFFFAOYSA-N chlorocyclohexatriene Chemical class ClC1=CC=C=C[CH]1 GEAXLHPORCRESC-UHFFFAOYSA-N 0.000 abstract 1
- 208000030381 cutaneous melanoma Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229950008696 farnesil Drugs 0.000 abstract 1
- 239000003102 growth factor Substances 0.000 abstract 1
- 210000003128 head Anatomy 0.000 abstract 1
- 210000004072 lung Anatomy 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 230000011278 mitosis Effects 0.000 abstract 1
- 210000000496 pancreas Anatomy 0.000 abstract 1
- 210000003800 pharynx Anatomy 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 abstract 1
- 201000003708 skin melanoma Diseases 0.000 abstract 1
Classifications
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- 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
- C07D401/10—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 aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A DERIVADOS DE QUINOLIN-2-ONA ALQUINIL SUSTITUIDOS DE FORMULA I, DONDE R1 ES H, ALQUILO C1-C10, (CR13R14)qCOR12, (CR13R14)qCOOR15, (CR13R14)qOR12, ENTRE OTROS; q ES 1-5; R2 ES HALO, CIANO, COOR15; R3, R4, R5, R6 Y R7 SON H, ALQUILO C1-C10, ALQUENILO C2-C10, HALO, CIANO, NITRO, ENTRE OTROS; R8 ES H, OR12, NR12R13, NR12COR13, CIANO, COOR13, SR12, (CR13R14)t(HETEROCICLO DE 4-10 MIEMBROS), R9 ES (CR13R14)t(IMIDAZOLILO); t ES 0-5; R12 ES H, ALQUILO C1-C10, (CR13R14)t(CICLOALQUILO C3-C10), (CR13R14)t(ARILO C6-C10), ENTRE OTROS; R13 Y R14 SON H, ALQUILO C1-C6; R15 ES R12 Y NO ES H; R16 ES R12 Y SiR17R18R19; R17, R18, R19 NO SON H; UNO DE R3, R4 Y R5 ES (CR13R14)tCCR16. SON COMPUESTOS PREFERIDOS 6-[(4-CLOROFENIL)HIDROXI-(3-METIL-3H-IMIDAZOL-4-IL)METIL]-4-(3-ETINILFENIL)-1-METIL-1H-QUINOLIN-2-ONA (ENANTIOMERO A o B), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS UN AGENTE ANTITUMORAL COMO INHIBIDORES DE MITOSIS, AGENTES ALQUILANTES, ANTIMETABOLITOS, ANTIBIOTICOS INTERCALANTES, INHIBIDORES DEL FACTOR DE CRECIMIENTO, ENTRE OTROS. EL COMPUESTO I INHIBE A LA FARNESIL TRANSFERASA Y PUEDE SER UTIL PARA EL TRATAMIENTO DEL DESARROLLO ANORMAL DE CELULAS, CANCER, DE PULMON, HUESOS, PANCREAS, PIEL, CABEZA, GARGANTA, MELANOMA CUTANEO; ENFERMEDAD PROLIFERATIVA BENIGNA COMO PSORIASIS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9814598P | 1998-08-27 | 1998-08-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20000986A1 true PE20000986A1 (es) | 2000-09-30 |
Family
ID=22267481
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1999000862A PE20000986A1 (es) | 1998-08-27 | 1999-08-26 | Derivados de quinolin-2-ona alquinilsustituidos utiles como agentes anticancerosos |
Country Status (40)
| Country | Link |
|---|---|
| US (3) | US6150377A (es) |
| EP (1) | EP1107963B1 (es) |
| JP (1) | JP3495706B2 (es) |
| KR (1) | KR20010072991A (es) |
| CN (1) | CN1314904A (es) |
| AP (1) | AP2001002079A0 (es) |
| AT (1) | ATE321037T1 (es) |
| AU (1) | AU4925499A (es) |
| BG (1) | BG105365A (es) |
| BR (1) | BRPI9913138B8 (es) |
| CA (2) | CA2341690C (es) |
| CO (1) | CO5130017A1 (es) |
| CZ (1) | CZ2001660A3 (es) |
| DE (1) | DE69930518T2 (es) |
| DZ (1) | DZ2880A1 (es) |
| EA (1) | EA200100135A1 (es) |
| EE (1) | EE200100118A (es) |
| ES (1) | ES2259237T3 (es) |
| GE (1) | GEP20033001B (es) |
| GT (1) | GT199900140A (es) |
| HK (1) | HK1039123A1 (es) |
| HR (1) | HRP20010142A2 (es) |
| HU (1) | HUP0103228A3 (es) |
| ID (1) | ID27562A (es) |
| IL (1) | IL141239A0 (es) |
| IS (1) | IS5818A (es) |
| MA (1) | MA26680A1 (es) |
| NO (1) | NO20010964L (es) |
| NZ (1) | NZ509372A (es) |
| OA (1) | OA11645A (es) |
| PA (1) | PA8480101A1 (es) |
| PE (1) | PE20000986A1 (es) |
| PL (1) | PL346426A1 (es) |
| SK (1) | SK2442001A3 (es) |
| SV (1) | SV1999000141A (es) |
| TN (1) | TNSN99162A1 (es) |
| TR (1) | TR200101343T2 (es) |
| UY (1) | UY25682A1 (es) |
| WO (1) | WO2000012499A1 (es) |
| ZA (1) | ZA200101173B (es) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030114503A1 (en) * | 1997-06-16 | 2003-06-19 | Pfizer Inc. | Farnesyl transferase inhibitors in combination with HMG CoA reductase inhibitors for the treatment of cancer |
| HRP20000904A2 (en) * | 1998-07-06 | 2001-12-31 | Janssen Pharmaceutica Nv | Farnesyl protein transferase inhibitors for treating arthropathies |
| ES2237125T3 (es) * | 1998-08-27 | 2005-07-16 | Pfizer Products Inc. | Derivados de quinolin-2-ona utiles como agentes anticancerigenos. |
| ATE321037T1 (de) * | 1998-08-27 | 2006-04-15 | Pfizer Prod Inc | Als antikrebsmittel verwendbare alkinyl- substituierte chinolin-2-on-derivate |
| ES2243228T3 (es) | 1999-02-11 | 2005-12-01 | Pfizer Products Inc. | Derivados quinolin-2-ona sustituidos con heteroarilo utiles como agentes anticancerigenos. |
| HN2000000266A (es) | 2000-01-21 | 2001-05-21 | Pfizer Prod Inc | Compuesto anticanceroso y metodo de separacion de enantiomeros util para sintetizar dicho compuesto. |
| DE60130976T2 (de) | 2000-02-24 | 2008-07-17 | Janssen Pharmaceutica N.V. | Dosierschema enthaldend farnesyl protein transferase inhibitoren für die behandlung von krebs |
| JO2361B1 (en) * | 2000-06-22 | 2006-12-12 | جانسين فارماسيوتيكا ان. في | Enaniumer 1,2-anylated quinoline inhibitor for the transporter - farnesyl |
| WO2002024682A1 (en) | 2000-09-25 | 2002-03-28 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors |
| AU2001293835A1 (en) | 2000-09-25 | 2002-04-02 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives |
| ES2313991T3 (es) * | 2000-09-25 | 2009-03-16 | Janssen Pharmaceutica Nv | Derivados de 6-heterociclilmetil-quinolina y quinazolina que inhiben la farnesil transferasa. |
| JP4974437B2 (ja) | 2000-09-25 | 2012-07-11 | 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6−[(置換フェニル)メチル]−キノリンおよびキナゾリン誘導体 |
| US7153958B2 (en) | 2000-11-21 | 2006-12-26 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting benzoheterocyclic derivatives |
| EP1395577A1 (en) * | 2000-12-19 | 2004-03-10 | Pfizer Products Inc. | Crystal forms of 6- (4-chloro-phenyl)-hydroxy-(-3-methyl-3h-imidaol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1h-quinolin-2-one, 2,3-dihydroxybutanedioate salts and method of production |
| WO2002051835A1 (en) * | 2000-12-27 | 2002-07-04 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 4-substituted quinoline and quinazoline derivatives |
| WO2002056884A2 (en) * | 2001-01-22 | 2002-07-25 | Schering Corporation | Treatment of malaria with farnesyl protein transferase inhibitors |
| AU2002253101B2 (en) * | 2001-03-12 | 2007-08-09 | Janssen Pharmaceutica N.V. | Process for the preparation of imidazole compounds |
| US20020151563A1 (en) * | 2001-03-29 | 2002-10-17 | Pfizer Inc. | Farnesyl transferase inhibitors in combination with HMG CoA reductase inhibitors for the inhibition of abnormal cell growth |
| AU2002257114A1 (en) * | 2001-04-06 | 2002-10-21 | Schering Corporation | Treatment of malaria with farsenyl protein transferase inhibitors |
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| 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 |
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| SI1784396T1 (sl) * | 2004-08-26 | 2011-03-31 | Pfizer | S pirazolom substituirane aminoheteroarilne spojine kot zaviralci protein-kinaze |
| SI2362218T1 (sl) | 2004-11-05 | 2014-12-31 | Janssen Pharmaceutica N.V. | Postopki za spremljanje učinkovitosti inhibitorjev farneziltransferaze |
| US20060107555A1 (en) * | 2004-11-09 | 2006-05-25 | Curtis Marc D | Universal snow plow adapter |
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| GEP20125398B (en) * | 2005-09-07 | 2012-02-27 | Amjen Freemont Ink | Human monoclonal antibodies to activin receptor-like kinase-1 |
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| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| ES2565238T3 (es) | 2006-04-20 | 2016-04-01 | Janssen Pharmaceutica N.V. | Inhibidores de la c-fms quinasa |
| CN101490046A (zh) | 2006-05-09 | 2009-07-22 | 辉瑞产品公司 | 环烷基氨基酸衍生物及其药物组合物 |
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| WO2008112525A2 (en) * | 2007-03-09 | 2008-09-18 | Link Medicine Corporation | Treatment of lysosomal storage diseases |
| JO3240B1 (ar) | 2007-10-17 | 2018-03-08 | Janssen Pharmaceutica Nv | c-fms مثبطات كيناز |
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| DE102008022221A1 (de) * | 2008-05-06 | 2009-11-12 | Universität des Saarlandes | Inhibitoren der humanen Aldosteronsynthase CYP11B2 |
| US20100331363A1 (en) * | 2008-11-13 | 2010-12-30 | Link Medicine Corporation | Treatment of mitochondrial disorders using a farnesyl transferase inhibitor |
| BRPI0920927A2 (pt) | 2008-11-13 | 2019-09-24 | Link Medicine Corp | derivados de azaquinolinona e usos dos mesmos |
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| US11471538B2 (en) | 2017-02-10 | 2022-10-18 | INSERM (Institut National de la Santéet de la Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway |
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| KR20200090982A (ko) | 2017-02-21 | 2020-07-29 | 쿠라 온콜로지, 인크. | 파르네실트랜스퍼라제 억제제를 사용하는 암 환자의 치료 방법 |
| JP7325400B2 (ja) | 2017-08-07 | 2023-08-14 | クラ オンコロジー, インコーポレイテッド | ファルネシルトランスフェラーゼ阻害剤を用いてがんを治療する方法 |
| US10806730B2 (en) | 2017-08-07 | 2020-10-20 | Kura Oncology, Inc. | Methods of treating cancer with farnesyltransferase inhibitors |
| WO2019113269A1 (en) | 2017-12-08 | 2019-06-13 | Kura Oncology, Inc. | Methods of treating cancer patients with farnesyltransferase inhibitors |
| CA3117968A1 (en) | 2018-11-01 | 2020-05-07 | Kura Oncology, Inc. | Methods of treating cancer with farnesyltransferase inhibitors |
| JP2022514654A (ja) | 2018-12-21 | 2022-02-14 | クラ オンコロジー, インコーポレイテッド | 扁平上皮癌のための治療法 |
| US20220142983A1 (en) | 2019-03-01 | 2022-05-12 | Kura Oncology, Inc. | Methods of treating cancer with farnesyltransferase inhibitors |
| TW202108170A (zh) | 2019-03-15 | 2021-03-01 | 美商庫拉腫瘤技術股份有限公司 | 以法呢基轉移酶(farnesyltransferase)抑制劑治療癌症患者之方法 |
| SG11202110472WA (en) | 2019-03-29 | 2021-10-28 | Kura Oncology Inc | Methods of treating squamous cell carcinomas with farnesyltransferase inhibitors |
| TW202102218A (zh) | 2019-04-01 | 2021-01-16 | 美商庫拉腫瘤技術股份有限公司 | 以法呢基(farnesyl)轉移酶抑制劑治療癌症的方法 |
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| WO2020223583A1 (en) | 2019-05-02 | 2020-11-05 | Kura Oncology, Inc. | Methods of treating acute myeloid leukemia with farnesyltransferase inhibitors |
| JP7718659B2 (ja) | 2019-08-16 | 2025-08-05 | チルドレンズ ホスピタル メディカル センター | Cdc42特異的阻害剤で対象を治療する方法 |
| WO2021155006A1 (en) | 2020-01-31 | 2021-08-05 | Les Laboratoires Servier Sas | Inhibitors of cyclin-dependent kinases and uses thereof |
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| US5747498A (en) * | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| TW349948B (en) * | 1995-10-31 | 1999-01-11 | Janssen Pharmaceutica Nv | Farnesyl transferase inhibiting 2-quinolone derivatives |
| WO1997021701A1 (en) * | 1995-12-08 | 1997-06-19 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives |
| ATE321037T1 (de) * | 1998-08-27 | 2006-04-15 | Pfizer Prod Inc | Als antikrebsmittel verwendbare alkinyl- substituierte chinolin-2-on-derivate |
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