CO5640038A2 - Macrociclos derivados de la quinazolina como agentes antiproliferativos - Google Patents
Macrociclos derivados de la quinazolina como agentes antiproliferativosInfo
- Publication number
- CO5640038A2 CO5640038A2 CO05119403A CO05119403A CO5640038A2 CO 5640038 A2 CO5640038 A2 CO 5640038A2 CO 05119403 A CO05119403 A CO 05119403A CO 05119403 A CO05119403 A CO 05119403A CO 5640038 A2 CO5640038 A2 CO 5640038A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- amino
- halo
- mono
- optionally substituted
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed systems
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
Abstract
1.- Un compuesto que posee la fórmulalas formas N-óxidos, las sales de adición aceptables para uso farmacéutico y las formas estereoquímicamente isómeras del mismo, donde:Z representa O, CH2, NH o S; en particular Z representa NH;Y representa -alquilo C3-C9-, -alquenilo C3-C9-, -alquinilo C3-C9-, -alquilo C3-C7-CO-NH- sustituido en forma optativa con amino, mono- o di(alquil C1-4)amino o alquiloxicarbonilamino C1-4-, -alquenil-C3-7-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C1-4)amino o alquiloxicarbonilamino C1-4-, -alquinil-C3-7-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C1-4)amino o alquiloxicarbonilamino C1-4-, -alquiloxi-C1-5- alquilo C1-5-, -alquil-C1-5-NR13-alquilo C1-5, -alquil-C1-5-NR14-CO-alquilo C1-5, -alquil-C1-5-CO-NR15-alquilo C1-5-, -alquil-C1-6-CO-NH-, -alquil-C1-6-NH-CO-, -aIquil-C1-3-NH-CS-Het20-, -alquil-C1-3-NH-CO-Het20-, -alquil-C1-2-CO-Het21-CO-, -Het22-CH2-CO-NH-alquilo C1-3-, -CO-NH-alquilo C1-6-, -NH-CO-alquilo C1-6-, -CO-alquilo C1-7, -alquil-C1-7-CO-, -alquil-C1-6-CO-alquilo C1-6-, -alquil-C1-2-NH-CO-CR16R17-NH-, -alquil-C1-2-CO-NH-CR18R19-CO-, -alquil-C1-2-CO-NR20-alquil-C1-3-CO-, -alquil-C1-2-NR21-CH2-CO-NH-alquilo C1-3- o -NR22-CO-alquil-C1-3-NH-;X1 representa una unión directa, O, -O-alquil-C1-2-, CO, -CO-alquilo C1-2-, NR11, -NR11-alquilo C1-2-, -CH2-, -O-N=CH- o -alquilo C1-2-;X2 representa una unión directa, O, -O-alquilo C1-2-, CO, -CO-alquilo C1-2-, NR12, -NR12-alquilo C1-2-, -CH2-, -O-N=CH- o -alquilo C1-2-;R1 representa hidrógeno, ciano, halo, hidroxi, formilo, alcoxi C1-6-, alquilo C1-6-, halo-fenil-carbonilamino-, alcoxi C1-6- sustituido con halo, ...
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0305723 | 2003-05-27 | ||
| EP0310266 | 2003-09-15 | ||
| EP0351061 | 2003-12-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5640038A2 true CO5640038A2 (es) | 2006-05-31 |
Family
ID=33493782
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO05119403A CO5640038A2 (es) | 2003-05-27 | 2005-11-24 | Macrociclos derivados de la quinazolina como agentes antiproliferativos |
Country Status (32)
| Country | Link |
|---|---|
| US (4) | US7648975B2 (es) |
| EP (2) | EP2305687A1 (es) |
| JP (1) | JP4887151B2 (es) |
| KR (1) | KR101143878B1 (es) |
| CN (1) | CN102718775B (es) |
| AR (2) | AR045687A1 (es) |
| AT (1) | ATE544454T1 (es) |
| AU (1) | AU2004243487B2 (es) |
| BR (1) | BRPI0410714B8 (es) |
| CA (1) | CA2525214C (es) |
| CL (1) | CL2004001267A1 (es) |
| CO (1) | CO5640038A2 (es) |
| CY (1) | CY1113002T1 (es) |
| DK (1) | DK1633365T3 (es) |
| EA (1) | EA009064B1 (es) |
| ES (1) | ES2381976T3 (es) |
| HK (1) | HK1176350A1 (es) |
| HR (1) | HRP20120351T1 (es) |
| IL (3) | IL172154A0 (es) |
| IS (1) | IS3030B (es) |
| JO (1) | JO2785B1 (es) |
| MX (1) | MXPA05012762A (es) |
| MY (1) | MY148633A (es) |
| NO (1) | NO334209B1 (es) |
| NZ (1) | NZ544154A (es) |
| PA (1) | PA8603801A1 (es) |
| PL (1) | PL1633365T3 (es) |
| PT (1) | PT1633365E (es) |
| SI (1) | SI1633365T1 (es) |
| TW (3) | TWI379835B (es) |
| UA (1) | UA84010C2 (es) |
| WO (1) | WO2004105765A1 (es) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2785B1 (en) | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| US7750160B2 (en) * | 2003-11-13 | 2010-07-06 | Ambit Biosciences Corporation | Isoxazolyl urea derivatives as kinase modulators |
| EA013904B1 (ru) | 2003-12-18 | 2010-08-30 | Янссен Фармацевтика Н.В. | Пиридо- и пиримидопиримидиновые производные в качестве антипролиферативных агентов |
| AU2004298784B2 (en) | 2003-12-18 | 2011-06-09 | Janssen Pharmaceutica N.V | 3-cyano-quinoline derivatives with antiproliferative activity |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| EP1854789B1 (en) | 2005-02-23 | 2013-10-09 | Shionogi & Co., Ltd. | Quinazoline derivative having tyrosine kinase inhibitory activity |
| GB0509227D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Intracellular enzyme inhibitors |
| JP5345388B2 (ja) * | 2005-06-30 | 2013-11-20 | 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 | 環式アニリノ−ピリジノトリアジン |
| EP2044084B1 (en) * | 2006-07-13 | 2016-02-17 | Janssen Pharmaceutica NV | Mtki quinazoline derivatives |
| JP2009242240A (ja) * | 2006-08-04 | 2009-10-22 | Mebiopharm Co Ltd | 含ホウ素キナゾリン誘導体 |
| SG174774A1 (en) | 2006-09-11 | 2011-10-28 | Curis Inc | Quinazoline based egfr inhibitors containing a zinc binding moiety |
| CA2662587C (en) * | 2006-09-11 | 2013-08-06 | Curis, Inc. | Quinazoline based egfr inhibitors |
| US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| CA2664145A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Use of a mt kinase inhibitor for treating or preventing brain cancer |
| WO2008049930A2 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | A method for profiling kinase inhibitors |
| BRPI0718021A2 (pt) * | 2006-10-27 | 2013-11-12 | Janssen Pharmaceutica Nv | Uso de mtki 1 para tratar ou prevenir câncer ósseo |
| EA200970419A1 (ru) * | 2006-10-27 | 2009-10-30 | Янссен Фармацевтика Нв | Микроциклические хиназолиновые производные в качестве ингибиторов vegfr3 |
| WO2008087736A1 (ja) * | 2007-01-19 | 2008-07-24 | Ube Industries, Ltd. | アラルキルオキシ又はヘテロアラルキルオキシ基を有する芳香族アミンの製法 |
| US8642067B2 (en) | 2007-04-02 | 2014-02-04 | Allergen, Inc. | Methods and compositions for intraocular administration to treat ocular conditions |
| JP5536647B2 (ja) | 2007-07-27 | 2014-07-02 | 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 | ピロロピリミジン |
| US8119616B2 (en) | 2007-09-10 | 2012-02-21 | Curis, Inc. | Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety |
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| PT2350075E (pt) | 2008-09-22 | 2014-06-09 | Array Biopharma Inc | Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase |
| SG10201914059WA (en) | 2008-10-22 | 2020-03-30 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
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| TWI406853B (zh) * | 2010-04-07 | 2013-09-01 | Dev Center Biotechnology | Ｅｇｆｒ與ｖｅｇｆｒ－２雙重抑制劑及其用途與製法 |
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| WO2013126015A1 (en) | 2012-02-23 | 2013-08-29 | N. V. Nutricia | Composition comprising non- digestible oligosaccharides |
| ES2621220T3 (es) * | 2012-03-06 | 2017-07-03 | Pfizer Inc. | Derivados macrocíclicos para el tratamiento de enfermedades proliferativas |
| CN104513253A (zh) * | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
| KR102256242B1 (ko) * | 2014-02-07 | 2021-05-26 | 엑시테라 파마슈티컬스 인코퍼레이티드 | 치료 화합물 및 조성물 |
| MA39822A (fr) | 2014-04-03 | 2018-02-06 | Janssen Pharmaceutica Nv | Dérivés de pyrimidine bicycle |
| MA39823A (fr) | 2014-04-03 | 2018-01-09 | Janssen Pharmaceutica Nv | Dérivés de pyridine macrocyclique |
| CN113354649A (zh) | 2014-11-16 | 2021-09-07 | 阵列生物制药公司 | 一种新的晶型 |
| EP3359526A4 (en) | 2015-10-05 | 2019-04-03 | The Trustees of Columbia University in the City of New York | ACTIVATORS OF AUTOPHAGIC FLOW AND PHOSPHOLIPASE D AND CLAIRANCE OF PROTEIN AGGREGATES COMPRISING TAU AND TREATMENT OF PROTEINEOPATHIES |
| CA3003153A1 (en) | 2015-10-26 | 2017-05-04 | Loxo Oncology, Inc. | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| US10716869B2 (en) | 2016-02-29 | 2020-07-21 | Oncodesign Sa | Radiolabeled macrocyclic EGFR inhibitor |
| PE20181888A1 (es) | 2016-04-04 | 2018-12-11 | Loxo Oncology Inc | Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| RU2745953C2 (ru) | 2016-05-18 | 2021-04-05 | Локсо Онколоджи, Инк. | Способ получения (s)-n-(5-((r)-2-(2,5-дифторфенил)пирролидин-1-ил)-пиразоло[1,5-a]пиримидин-3-ил)-3-гидроксипирролидин-1-карбоксамида и его солей |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| KR20200096941A (ko) | 2017-12-07 | 2020-08-14 | 앰플릭스 파마슈티컬스, 인크. | 헤테로사이클 치환된 피리딘 유도체 항진균제 |
| JP2021530445A (ja) | 2018-06-25 | 2021-11-11 | アンプリックス ファーマシューティカルズ，インク． | 複素環およびアミノ基によって置換されたピリジン誘導体 |
| US20230159556A1 (en) * | 2020-04-20 | 2023-05-25 | Tenova Pharmaceuticals Inc. | Novel protein kinase inhibitors |
| TW202333709A (zh) | 2021-12-16 | 2023-09-01 | 美商奇奈特生物製藥公司 | Met激酶抑制劑 |
| WO2024017258A1 (zh) * | 2022-07-19 | 2024-01-25 | 百极弘烨(南通)医药科技有限公司 | Egfr小分子抑制剂、含其的药物组合物及其用途 |
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| DE2423536A1 (de) * | 1974-05-15 | 1975-11-27 | Bayer Ag | 3-amino-phenylessigsaeure-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide |
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-
2004
- 2004-05-24 JO JO200466A patent/JO2785B1/en active
- 2004-05-24 PA PA20048603801A patent/PA8603801A1/es unknown
- 2004-05-25 EA EA200501866A patent/EA009064B1/ru unknown
- 2004-05-25 NZ NZ544154A patent/NZ544154A/en unknown
- 2004-05-25 WO PCT/EP2004/005621 patent/WO2004105765A1/en active Application Filing
- 2004-05-25 BR BRPI0410714A patent/BRPI0410714B8/pt not_active Application Discontinuation
- 2004-05-25 SI SI200431864T patent/SI1633365T1/sl unknown
- 2004-05-25 EP EP10192741A patent/EP2305687A1/en not_active Withdrawn
- 2004-05-25 PL PL04739341T patent/PL1633365T3/pl unknown
- 2004-05-25 MY MYPI20042004A patent/MY148633A/en unknown
- 2004-05-25 CN CN201210144221.7A patent/CN102718775B/zh active Active
- 2004-05-25 ES ES04739341T patent/ES2381976T3/es active Active
- 2004-05-25 PT PT04739341T patent/PT1633365E/pt unknown
- 2004-05-25 CA CA2525214A patent/CA2525214C/en active Active
- 2004-05-25 JP JP2006529915A patent/JP4887151B2/ja active Active
- 2004-05-25 DK DK04739341.8T patent/DK1633365T3/da active
- 2004-05-25 MX MXPA05012762A patent/MXPA05012762A/es active IP Right Grant
- 2004-05-25 EP EP04739341A patent/EP1633365B1/en active Active
- 2004-05-25 AT AT04739341T patent/ATE544454T1/de active
- 2004-05-25 UA UAA200510181A patent/UA84010C2/ru unknown
- 2004-05-25 US US10/558,007 patent/US7648975B2/en active Active
- 2004-05-25 CL CL200401267A patent/CL2004001267A1/es unknown
- 2004-05-25 KR KR1020057022189A patent/KR101143878B1/ko active IP Right Grant
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2012
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