AR083213A1 - Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlos - Google Patents

Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlos

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Publication number
AR083213A1
AR083213A1 ARP110103595A ARP110103595A AR083213A1 AR 083213 A1 AR083213 A1 AR 083213A1 AR P110103595 A ARP110103595 A AR P110103595A AR P110103595 A ARP110103595 A AR P110103595A AR 083213 A1 AR083213 A1 AR 083213A1
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AR
Argentina
Prior art keywords
substituted
unsubstituted
formula
compound
hydrogen
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ARP110103595A
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English (en)
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Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44773179&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR083213(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR083213A1 publication Critical patent/AR083213A1/es

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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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

Se refiere además a procesos de elaboración para formas sólidas específicas del compuesto de fórmula (4) y sus sales, a estas formas sólidas, y al uso de tales formas sólidas para el tratamiento terapéutico de animales de sangre caliente.Reivindicación 1: Un proceso para la elaboración de un compuesto de la formula (1) o un estereoisómero, tautómero, o una sal del mismo, en donde: W es CRw o N, en donde Rw se selecciona a partir del grupo que consiste en hidrógeno, ciano, halógeno, metilo, trifluorometilo, sulfonamido; R1 se selecciona a partir del grupo que consiste en hidrógeno, ciano, nitro, halógeno, alquilo sustituido e insustituido, alquenilo sustituido e insustituido, alquinilo sustituido e insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, cicloalquilo sustituido e insustituido, -COR1a, -CO2R1a, -CONR1aR1b, -NR1aR1b, -NR1aSO2R1b, -OCOR1a, -OR1a, -SOR1a, en donde R1a y R1b se seleccionan independientemente a partir del grupo que consiste en hidrógeno, alquilo sustituido o insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, y cicloalquilo sustituido e insustituido; R2 selecciona a partir del grupo que consiste en hidrógeno, ciano, nitro, halógeno, hidroxilo, amino, alquilo sustituido e insustituido, -COR2a y -NR2aCOR2b, en donde R2a y R2b se seleccionan independientemente a partir del grupo que consiste en hidrógeno, y alquilo sustituido o insustituido; R3 se selecciona a partir del grupo que consiste en hidrógeno, ciano, nitro, halógeno, alquilo sustituido e insustituido, alquenilo sustituido e insustituido, alquinilo sustituido e insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, cicloalquilo sustituido e insustituido, -COR3a, -NR3aR3b, -NR3aCOR3b, -NR3aSO2R3b, -OR3a, -SR3a, -SOR3a, -SO2R3a, y en donde R3a y R3b se seleccionan independientemente a partir del .grupo que consiste en hidrógeno, alquilo sustituido o insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, y cicloalquilo sustituido e insustituido; y R4 se selecciona a partir del grupo que consiste en hidrógeno, y halógeno; el cual comprende el paso de hacer reaccionar un compuesto de la fórmula (2) en donde Y2B- representa un ácido borónico acíclico, un éster borónico acíclico o un éster borónico cíclico, R1 y R2 son como se definen para la fórmula (1), con un compuesto de la fórmula (3) en donde Hal representa halógeno, W, R3 y R4 son como se definen para un compuesto de la fórmula (1); bajo condiciones de Suzuki, para obtener un compuesto de la fórmula (1); opcionalmente seguido por una reacción de formación de sal. Reivindicación 7: Una forma cristalina del compuesto de la fórmula (4) o de un hidrato o solvato del compuesto de la fórmula (4), o de una sal del compuesto de la fórmula (4), o de un hidrato o solvato de una sal del compuesto de la fórmula (4). Reivindicación 9: Una forma cristalina del compuesto de fórmula (4) de acuerdo con la reivindicación 7, en la forma polimorfa A anhidra, en donde la forma cristalina del compuesto de fórmula (4) muestra, en la difracción de rayos-X, un pico en un ángulo de difracción 2q de 14.8 ± 0.3º y 10.2 ± 0.3º.
ARP110103595A 2010-10-01 2011-09-29 Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlos AR083213A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38872110P 2010-10-01 2010-10-01
US201161494915P 2011-06-09 2011-06-09

Publications (1)

Publication Number Publication Date
AR083213A1 true AR083213A1 (es) 2013-02-06

Family

ID=44773179

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103595A AR083213A1 (es) 2010-10-01 2011-09-29 Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlos

Country Status (31)

Country Link
US (3) US9181215B2 (es)
EP (2) EP3040333B1 (es)
JP (3) JP5998145B2 (es)
KR (2) KR20180123586A (es)
CN (3) CN104945373A (es)
AR (1) AR083213A1 (es)
AU (4) AU2011308856B2 (es)
BR (1) BR112013007123B1 (es)
CA (1) CA2813333C (es)
CL (2) CL2013000850A1 (es)
CO (1) CO6700837A2 (es)
DK (1) DK3040333T3 (es)
EC (1) ECSP13012596A (es)
ES (1) ES2699951T3 (es)
GT (1) GT201300080A (es)
HK (1) HK1220686A1 (es)
HU (1) HUE041326T2 (es)
IL (3) IL225113A (es)
LT (1) LT3040333T (es)
MX (1) MX354482B (es)
MY (1) MY160785A (es)
NZ (1) NZ608285A (es)
PE (1) PE20140002A1 (es)
PH (1) PH12015501585A1 (es)
PL (1) PL3040333T3 (es)
PT (1) PT3040333T (es)
RU (2) RU2015150728A (es)
SG (1) SG188439A1 (es)
SI (1) SI3040333T1 (es)
TW (1) TWI540133B (es)
WO (1) WO2012044727A2 (es)

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ES2676180T3 (es) 2011-07-01 2018-07-17 Novartis Ag Terapia de combinación que comprende un inhibidor de CDK4/6 y un inhibidor de PI3K para el uso en el tratamiento de cáncer
KR20140069235A (ko) 2011-09-27 2014-06-09 노파르티스 아게 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
KR102128127B1 (ko) * 2012-10-23 2020-06-30 노파르티스 아게 5-(2,6-디-4-모르폴리닐-4-피리미디닐)-4-트리플루오로메틸피리딘-2-아민의 개선된 제조 방법
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
EA028033B1 (ru) 2013-03-14 2017-09-29 Новартис Аг 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантного idh
US9318944B2 (en) 2013-04-29 2016-04-19 Rockwell Automation Technologies, Inc. Methods and apparatus for active front end filter capacitor degradation detection
US9294005B2 (en) 2013-10-01 2016-03-22 Rockwell Automation Technologies, Inc. Method and apparatus for detecting AFE filter capacitor degradation
RU2663999C2 (ru) * 2013-10-16 2018-08-14 Шанхай Инли Фармасьютикал Ко., Лтд Конденсированное гетероциклическое соединение, способ его получения, его фармацевтическая композиция и применения
US10100031B2 (en) * 2014-04-22 2018-10-16 Universitaet Basel Manufacturing process for triazine, pyrimidine and pyridine derivatives
CN105085476B (zh) * 2014-11-24 2018-03-09 苏州晶云药物科技有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法
CA2971118C (en) 2014-12-17 2020-07-14 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof
US9481665B2 (en) * 2015-03-13 2016-11-01 Yong Xu Process for preparing PI3K inhibitor buparsilib
JP2018509448A (ja) 2015-03-25 2018-04-05 ノバルティス アーゲー 組合せ医薬
CN105001151B (zh) * 2015-08-28 2017-07-14 苏州明锐医药科技有限公司 布帕尼西中间体及其制备方法
CN106543140A (zh) * 2015-09-21 2017-03-29 苏州晶云药物科技有限公司 5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺盐酸盐的晶型及其制备方法
DK3389662T3 (da) * 2015-12-16 2022-02-28 Genentech Inc Fremgangsmåde til fremstilling af tricykliske PI3K-inhibitorforbindelser og fremgangsmåder til anvendelse af disse til behandling af cancer
CN106905294A (zh) * 2016-07-08 2017-06-30 苏州科睿思制药有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法
CN107793394A (zh) * 2017-08-03 2018-03-13 上海厚璞生物科技有限公司 一种生产选择性pi3k抑制剂的系列关键中间体
CN110016142B (zh) * 2019-04-30 2021-08-03 合肥工业大学 一种含嘧啶硼酸结构的硅油及其制备方法

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CN1735598A (zh) * 2002-11-11 2006-02-15 拜耳医药保健股份公司 作为ip受体拮抗剂的苯基或杂芳基氨基烷烃衍生物
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JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
KR101435231B1 (ko) 2006-08-24 2014-10-02 아스트라제네카 아베 증식성 질환의 치료에 유용한 모르폴리노 피리미딘 유도체
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JP2016106091A (ja) 2016-06-16
AU2011308856B2 (en) 2015-04-23
ECSP13012596A (es) 2013-07-31
SG188439A1 (en) 2013-05-31
KR20180123586A (ko) 2018-11-16
GT201300080A (es) 2014-07-18
CN104987321A (zh) 2015-10-21
TW201215605A (en) 2012-04-16
MX2013003507A (es) 2013-05-20
WO2012044727A2 (en) 2012-04-05
IL233282A (en) 2016-08-31
PE20140002A1 (es) 2014-01-21
MX354482B (es) 2018-03-07
NZ608285A (en) 2014-06-27
CL2015001088A1 (es) 2015-07-10
JP5998145B2 (ja) 2016-09-28
AU2015246141A1 (en) 2015-11-12
AU2015246141B2 (en) 2016-07-07
US20160251334A1 (en) 2016-09-01
CL2013000850A1 (es) 2013-09-27
TWI540133B (zh) 2016-07-01
AU2015200936A1 (en) 2015-03-12
CN104945373A (zh) 2015-09-30
KR20130119928A (ko) 2013-11-01
EP3040333A1 (en) 2016-07-06
PH12015501585A1 (en) 2015-09-21
IL238046A (en) 2016-08-31
IL225113A (en) 2016-08-31
RU2576619C2 (ru) 2016-03-10
AU2015200938B2 (en) 2015-11-19
JP2016128414A (ja) 2016-07-14
HK1220686A1 (zh) 2017-05-12
CA2813333A1 (en) 2012-04-05
US20130225571A1 (en) 2013-08-29
CA2813333C (en) 2019-01-15
US20150232446A1 (en) 2015-08-20
LT3040333T (lt) 2018-12-10
DK3040333T3 (da) 2019-01-02
US9181215B2 (en) 2015-11-10
CO6700837A2 (es) 2013-06-28
MY160785A (en) 2017-03-15
AU2011308856A1 (en) 2013-03-28
BR112013007123A2 (pt) 2016-06-14
RU2015150728A (ru) 2019-01-15
PT3040333T (pt) 2018-12-04
RU2013120326A (ru) 2014-11-20
AU2015200938A1 (en) 2015-03-12
JP2013541536A (ja) 2013-11-14
CN103140479B (zh) 2015-04-08
PL3040333T3 (pl) 2019-03-29
HUE041326T2 (hu) 2019-05-28
US9452994B2 (en) 2016-09-27
EP2621908A2 (en) 2013-08-07
IL233282A0 (en) 2014-08-31
US9359326B2 (en) 2016-06-07
EP3040333B1 (en) 2018-09-12
CN103140479A (zh) 2013-06-05
SI3040333T1 (sl) 2019-01-31
BR112013007123B1 (pt) 2021-11-09
WO2012044727A3 (en) 2012-06-07
ES2699951T3 (es) 2019-02-13

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