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PE20090835A1 - Derivados de quinazolina como inhibidores de la pi3 quinasa - Google Patents

Derivados de quinazolina como inhibidores de la pi3 quinasa

Info

Publication number
PE20090835A1
PE20090835A1 PE2008001006A PE2008001006A PE20090835A1 PE 20090835 A1 PE20090835 A1 PE 20090835A1 PE 2008001006 A PE2008001006 A PE 2008001006A PE 2008001006 A PE2008001006 A PE 2008001006A PE 20090835 A1 PE20090835 A1 PE 20090835A1
Authority
PE
Peru
Prior art keywords
quinazoline derivatives
kinase inhibitors
quinazolinyl
pyridinyl
heteroaryl
Prior art date
Application number
PE2008001006A
Other languages
English (en)
Inventor
Nicholas D Adams
Joelle Lorraine Burgess
Michael Gerard Darcy
Steven David Knight
Kenneth Allen Newlander
Lance H Ridgers
Stanley J Schmidt
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40156899&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20090835(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20090835A1 publication Critical patent/PE20090835A1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
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  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
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Abstract

REFERIDO A DERIVADOS DE QUINAZOLINAS DE FORMULA I DONDE R2 ES ARILO, HETEROARILO SUSTITUIDO O NO; R1 ES HETEROCICLOALQUILO, HETEROARILO, ARILO, ENTRE OTROS; R3 Y R4 SON CADA UNO H, HALOGENO, ACILO, ENTRE OTROS; n ES 1-2. SON COMPUESTOS PREFERIDOS: 4-(4-PIRIDINIL)-6-(1H-PIRROLO[2,3-b]PIRIDIN-5-IL)QUINAZOLINA; 5-[4-(1-PIPERIDINIL)-6-QUINAZOLINIL]-3-PIRIDINASULFONAMIDA; N-{2-CLORO-5-[4-(4-MORFOLINIL)-6-QUINAZOLINIL]3-PIRIDINIL}-N-METILETANOSULFONAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE PREPARACION Y A UN METODO DE TRATAMIENTO. DICHO COMPUESTO INHIBE LA ACTIVIDAD/FUNCION DE QUINASAS PI3 Y ES UTIL EN EL TRATAMIENTO DE TRASTORNOS AUTOINMUNES, ALERGIA, ASMA, ENTRE OTROS
PE2008001006A 2007-06-14 2008-06-12 Derivados de quinazolina como inhibidores de la pi3 quinasa PE20090835A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94389907P 2007-06-14 2007-06-14

Publications (1)

Publication Number Publication Date
PE20090835A1 true PE20090835A1 (es) 2009-07-25

Family

ID=40156899

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001006A PE20090835A1 (es) 2007-06-14 2008-06-12 Derivados de quinazolina como inhibidores de la pi3 quinasa

Country Status (9)

Country Link
US (2) US20100179144A1 (es)
EP (1) EP2167092A4 (es)
JP (1) JP2010532320A (es)
AR (1) AR066978A1 (es)
CL (1) CL2008001743A1 (es)
PE (1) PE20090835A1 (es)
TW (1) TW200918068A (es)
UY (1) UY31137A1 (es)
WO (1) WO2008157191A2 (es)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
CA2694136C (en) 2007-08-02 2013-09-17 Amgen Inc. Pi3 kinase modulators and methods of use
JP2011500823A (ja) * 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体
WO2009085230A1 (en) 2007-12-19 2009-07-09 Amgen Inc. Inhibitors of pi3 kinase
MX315904B (es) 2008-05-30 2013-11-29 Amgen Inc Inhibidores de fosfoinosituro-3 cinasa.
RU2011123647A (ru) 2008-11-10 2012-12-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, полезные в качестве ингибиторов atr киназы
AU2009327357C1 (en) 2008-12-19 2017-02-02 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of ATR kinase
SG173155A1 (en) * 2009-02-12 2011-08-29 Merck Serono Sa 2-morpholino-pyrido[3,2-d]pyrimidines
SI2429995T1 (sl) 2009-05-15 2014-05-30 Novartis Ag Arilpiridini kot inhibitorji aldosteron sintaze
KR20130066633A (ko) 2010-05-12 2013-06-20 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
JP2013529200A (ja) 2010-05-12 2013-07-18 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011143399A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569289A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
MX2012013082A (es) 2010-05-12 2013-05-09 Vertex Pharma Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr.
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
DE102010049595A1 (de) * 2010-10-26 2012-04-26 Merck Patent Gmbh Chinazolinderivate
WO2012125668A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CA2832100A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
WO2012178124A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
CN103957917A (zh) 2011-09-30 2014-07-30 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CA3124539A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Process for making 4-[chloro-n-hydroxycarbonimidoyl]phenyl derivative
WO2013049722A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2014530851A (ja) * 2011-10-21 2014-11-20 ノバルティスアーゲー Pi3kモジュレータとしてのキナゾリン誘導体
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841337B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US9949979B2 (en) * 2011-12-15 2018-04-24 Novartis Ag Use of inhibitors of the activity or function of PI3K
CA2861496A1 (en) * 2012-02-06 2013-08-15 Glaxosmithkline Intellectual Property (No.2) Limited Pi3k inhibitors for treating cough
WO2013117503A2 (en) 2012-02-06 2013-08-15 Glaxosmithkline Intellectual Property (No. 2) Limited Novel use
US20140044802A1 (en) 2012-04-05 2014-02-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
CN102746241B (zh) * 2012-07-02 2014-11-05 西安交通大学 2,3,5-三取代苯甲酰胺类化合物及其制备方法和用途
EP2904406B1 (en) 2012-10-04 2018-03-21 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
HK1211027A1 (en) 2012-10-16 2016-05-13 Almirall, S.A. Pyrrolotriazinone derivatives as pi3k inhibitors
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
RS64234B1 (sr) 2012-12-07 2023-06-30 Vertex Pharma Pirazolo[1,5-a]pirimidini korisni kao inhibitori atr kinaze za lečenje kancera
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2909310A1 (en) 2013-04-12 2014-10-16 Asana Biosciences, Llc Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways
SI3077397T1 (sl) 2013-12-06 2020-02-28 Vertex Pharmaceuticals Inc. 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)pirazolo(1,5-A)pirimidin-3- karboksamidna spojina, koristna kot inhibitor kinaze ATR, njena priprava, različne trdne oblike in njeni radioaktivno označeni derivati
CR20160363A (es) 2014-01-14 2016-10-12 Millennium Pharm Inc Heteroarilos y usos de estos
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
EP3110801B1 (en) 2014-02-27 2019-01-30 Council Of Scientific & Industrial Research 6-aryl-4-phenylamino-quinazoline analogs as phosphoinositide-3-kinase inhibitors
JP2017512776A (ja) * 2014-03-15 2017-05-25 ウェイク フォレスト ユニバーシティ 貴金属求電子体で修飾された官能化チロシンキナーゼ阻害剤およびそれと関連した方法
SG11201610197XA (en) 2014-06-05 2017-01-27 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
NZ727399A (en) 2014-06-17 2022-07-29 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
US10206924B2 (en) * 2014-12-15 2019-02-19 The Regents Of The University Of Michigan Small molecule inhibitors of EGFR and PI3K
CN105237484B (zh) * 2015-09-28 2018-12-07 西安交通大学 一种6-芳基取代的喹啉类化合物及其应用
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
CN108239076B (zh) * 2016-12-26 2021-07-06 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
CN108239075B (zh) * 2016-12-26 2021-07-02 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
CN108239074B (zh) * 2016-12-26 2021-07-06 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
CA3048546A1 (en) 2016-12-26 2018-07-05 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Quinazoline compound and preparation method, application, and pharmaceutical compostion thereof
CN108727342A (zh) * 2017-04-21 2018-11-02 沈阳药科大学 4-芳氨-6-(3-磺酰胺基吡啶)-喹唑啉类衍生物及其制备方法和应用
CN108976197A (zh) * 2017-06-02 2018-12-11 沈阳药科大学 4-烷氨基-喹唑啉类衍生物及其制备方法和应用
CN108373462A (zh) * 2017-12-22 2018-08-07 西安交通大学 6-(吡啶-4-基)-4-取代氨基的喹唑啉或喹啉类化合物及其应用
CN112341434B (zh) * 2019-08-08 2021-11-26 恩瑞生物医药科技(上海)有限公司 PI3K/mTOR蛋白降解靶向嵌合体类化合物及其制备方法和医药用途
EP4267554A1 (en) 2020-12-22 2023-11-01 Mekanistic Therapeutics LLC Substituted aminobenzyl heteroaryl compounds as egfr and/or pi3k inhibitors
CN113416181B (zh) * 2021-08-02 2022-05-03 四川大学 喹唑啉类衍生物及其用途

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
EP0837063A1 (en) * 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
HRP20020838A2 (en) * 2000-04-25 2004-12-31 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
EP1512413A3 (en) * 2001-01-16 2009-09-23 Glaxo Group Limited Pharmaceutical combination containing a 4-quinazolineamine and another anti-neoplastic agent for the treatment of cancer
DE60203260T2 (de) * 2001-01-16 2006-02-02 Glaxo Group Ltd., Greenford Pharmazeutische kombination, die ein 4-chinazolinamin und paclitaxel, carboplatin oder vinorelbin enthält, zur behandlung von krebs
EP2048142A3 (en) * 2001-04-26 2009-04-22 Eisai R&D Management Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
WO2004004732A1 (en) * 2002-07-09 2004-01-15 Astrazeneca Ab Quinazoline derivatives for use in the treatment of cancer
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
WO2006071875A1 (en) * 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
JP5079500B2 (ja) * 2005-04-28 2012-11-21 協和発酵キリン株式会社 2−アミノキナゾリン誘導体
US7989461B2 (en) * 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
CN101003514A (zh) * 2006-01-20 2007-07-25 上海艾力斯医药科技有限公司 喹唑啉衍生物、其制备方法及用途
TW200808739A (en) * 2006-04-06 2008-02-16 Novartis Vaccines & Diagnostic Quinazolines for PDK1 inhibition
PL2049502T3 (pl) * 2006-07-28 2012-06-29 Novartis Ag 2,4-Podstawione chinazoliny jako inhibitory kinazy lipidowej
MX2009006627A (es) * 2006-12-22 2009-08-12 Novartis Ag Quinazolinas para la inhibicion de pdk1.
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
JP2011500823A (ja) * 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体

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