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PE20110147A1 - Composicion y proceso - 356 - Google Patents

Composicion y proceso - 356

Info

Publication number
PE20110147A1
PE20110147A1 PE2010001171A PE2010001171A PE20110147A1 PE 20110147 A1 PE20110147 A1 PE 20110147A1 PE 2010001171 A PE2010001171 A PE 2010001171A PE 2010001171 A PE2010001171 A PE 2010001171A PE 20110147 A1 PE20110147 A1 PE 20110147A1
Authority
PE
Peru
Prior art keywords
pyrimidin
salt
metoxybenzyl
metoxifenil
methylmorpholin
Prior art date
Application number
PE2010001171A
Other languages
English (en)
Inventor
Helen Blade
Gwydion Huw Churchill
Angela Charlotte Currie
Benjamin Charles Dobson
Peter Samuel Hynes
Martin Neal Kenworthy
Lyn Powel
Steven Anthony Raw
Original Assignee
Astrazeneca Ab
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
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20110147A1 publication Critical patent/PE20110147A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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

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)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A UN PROCESO PARA PREPARAR COMPUESTOS DERIVADOS DE (5-{2,4-bis[(3S)-3-METILMORFOLIN-4-IL]PIRIDO[2,3-d]PIRIMIDIN-7-IL}-2-METOXIFENIL)METANOL Y SUS SALES FOSFATO, SULFATO, MALATO, ENTRE OTROS; QUE COMPRENDE: A) REACCION DE UNA SAL DE 5-[(2E)-3-(DIMETILAMINO)PROP-2-ENOIL]-2-METOXIBENCILO DEL ACIDO PIVALICO O ESTER METILICO CON UN URACILO SUSTITUIDO EN LA POSICION 6 PARA OBTENER UNA SAL DE 5- (2,4-DIOXO-1,2,3,4-TETRAHIDROPIRIDO[2,3-d]PIRIMIDIN-7-IL)-2-METOXIBENCILO; B) REACCION DEL OBTENIDO CON UN AGENTE HALOGENANTE PARA OBTENER UNA SAL DE 5-(2,4-DIHALOPIRIDO[2,3-d]PIRIMIDIN-7-IL)-2-METOXIBENCILO; C) HACER REACCIONAR EL OBTENIDO CON METILMORFOLINA; D) ELIMINAR LOS GRUPOS PROTECTORES PARA OBTENER EL COMPUESTO (5-{2,4-bis[(3S)-3-METILMORFOLIN-4-IL]PIRIDO[2,3-d]PIRIMIDIN-7-IL}-2-METOXIFENIL)METANOL. ADICIONALMENTE SE PUEDE AISLAR EL COMPUESTO EN MENCION COMO UNA SAL. TAMBIEN REFIERE A UNA FORMULACION FARMACEUTICA. DICHO PROCESO ES UTIL PARA PREPARAR COMPUESTOS INHIBIDORES DE LA QUINASA mTOR UTIL EN EL TRATAMIENTO DE UNA ENFERMEDAD PROLIFERATIVA COMO EL CANCER
PE2010001171A 2008-06-20 2009-06-18 Composicion y proceso - 356 PE20110147A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7418808P 2008-06-20 2008-06-20
US15235009P 2009-02-13 2009-02-13

Publications (1)

Publication Number Publication Date
PE20110147A1 true PE20110147A1 (es) 2011-03-26

Family

ID=41051136

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2010001171A PE20110147A1 (es) 2008-06-20 2009-06-18 Composicion y proceso - 356

Country Status (26)

Country Link
US (1) US8198441B2 (es)
EP (1) EP2303875B1 (es)
JP (1) JP5607614B2 (es)
KR (1) KR101668497B1 (es)
CN (1) CN102137860B (es)
AR (1) AR072263A1 (es)
AU (1) AU2009261688B2 (es)
BR (1) BRPI0914912A2 (es)
CA (1) CA2728183C (es)
CL (1) CL2010001488A1 (es)
CO (1) CO6351729A2 (es)
CR (1) CR11859A (es)
DO (1) DOP2010000391A (es)
EA (1) EA019092B1 (es)
EC (1) ECSP10010696A (es)
ES (1) ES2398423T3 (es)
IL (1) IL210074A (es)
MX (1) MX2010014230A (es)
MY (1) MY172107A (es)
NI (1) NI201000225A (es)
PE (1) PE20110147A1 (es)
SV (1) SV2010003770A (es)
TW (1) TWI441821B (es)
UY (1) UY31917A (es)
WO (1) WO2009153597A2 (es)
ZA (1) ZA201101861B (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2715181A1 (en) * 2008-02-21 2009-08-27 Astrazeneca Ab Combination therapy 238
EP3053925A1 (en) 2010-12-16 2016-08-10 F. Hoffmann-La Roche AG Tricyclic pi3k inhibitor compounds and methods of use
CN104803922A (zh) * 2015-03-14 2015-07-29 长沙深橙生物科技有限公司 一种嘧啶衍生物的制备方法
CN106008559B (zh) * 2015-03-25 2020-10-16 中国科学院上海药物研究所 取代吡啶并嘧啶类化合物的合成工艺
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
WO2019157516A1 (en) 2018-02-12 2019-08-15 resTORbio, Inc. Combination therapies
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib
SG11202012447YA (en) 2018-06-15 2021-01-28 Navitor Pharm Inc Rapamycin analogs and uses thereof
TW202134234A (zh) 2019-12-05 2021-09-16 美商奈維特製藥公司 雷帕黴素類似物及其用途

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4560685A (en) * 1984-06-18 1985-12-24 Dr. Karl Thomae Gesellschaft Mit Beschrankter Haftung 2-Piperazino-pteridines useful as antithrombotics and antimetastatics
DE3445298A1 (de) 1984-12-12 1986-06-12 Dr. Karl Thomae Gmbh, 7950 Biberach Neue pteridine, verfahren zu ihrer herstellung und deren verwendung als zwischenprodukte oder als arzneimittel
US5990117A (en) * 1998-04-15 1999-11-23 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to quinazoline derivatives
DK1481970T3 (da) 1999-09-07 2006-07-31 Syngenta Participations Ag Nye herbicider
CN1186324C (zh) 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
US20030187026A1 (en) * 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
SI1575951T1 (sl) 2002-12-06 2014-10-30 Debiopharm International Sa Forum "Apres-Demain" Heterociklične spojine, postopki za njihovo izdelavo in njihova uporaba v terapiji
ES2290743T3 (es) 2003-04-30 2008-02-16 The Institutes For Pharmaceutical Discovery, Llc Heteroarilos sustituidos como inhibidores de las proteina-tirosina fosfatasas.
GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
EP1899332A1 (en) 2005-06-24 2008-03-19 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c.
US20070128658A1 (en) * 2005-11-14 2007-06-07 Blackwell Helen E Fluorescent dyes, methods and uses thereof
CA2628920C (en) * 2005-11-22 2015-12-29 Kudos Pharmaceuticals Limited Pyrido-,pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
AU2007287430B2 (en) * 2006-08-23 2011-07-21 Kudos Pharmaceuticals Limited 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mTOR inhibitors
BRPI0818426A2 (pt) * 2007-10-15 2017-06-13 Astrazeneca Ab produto de combinação, uso de um produto de combinação, e, método para tratar câncer

Also Published As

Publication number Publication date
MX2010014230A (es) 2011-03-29
CA2728183A1 (en) 2009-12-23
EA201100063A1 (ru) 2011-10-31
AR072263A1 (es) 2010-08-18
US20090318434A1 (en) 2009-12-24
WO2009153597A3 (en) 2010-05-06
IL210074A (en) 2015-07-30
TW201012818A (en) 2010-04-01
MY172107A (en) 2019-11-14
BRPI0914912A2 (pt) 2017-06-20
AU2009261688A1 (en) 2009-12-23
CN102137860B (zh) 2013-08-28
ES2398423T3 (es) 2013-03-19
US8198441B2 (en) 2012-06-12
AU2009261688B2 (en) 2012-07-05
NI201000225A (es) 2011-12-15
ZA201101861B (en) 2011-11-30
HK1155160A1 (en) 2012-05-11
CO6351729A2 (es) 2011-12-20
CR11859A (es) 2011-02-25
EA019092B1 (ru) 2014-01-30
KR20110027789A (ko) 2011-03-16
CL2010001488A1 (es) 2011-07-15
WO2009153597A2 (en) 2009-12-23
IL210074A0 (en) 2011-02-28
ECSP10010696A (es) 2011-01-31
EP2303875B1 (en) 2012-11-28
EP2303875A2 (en) 2011-04-06
DOP2010000391A (es) 2011-01-15
CN102137860A (zh) 2011-07-27
TWI441821B (zh) 2014-06-21
KR101668497B1 (ko) 2016-10-21
UY31917A (es) 2010-01-29
CA2728183C (en) 2016-10-25
SV2010003770A (es) 2011-05-20
JP5607614B2 (ja) 2014-10-15
JP2011524889A (ja) 2011-09-08

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Legal Events

Date Code Title Description
FA Abandonment or withdrawal