ECSP13012596A - Proceso de elaboración para derivados de pirimidina - Google Patents

Proceso de elaboración para derivados de pirimidina

Info

Publication number
ECSP13012596A
ECSP13012596A ECSP13012596A ECSP13012596A EC SP13012596 A ECSP13012596 A EC SP13012596A EC SP13012596 A ECSP13012596 A EC SP13012596A EC SP13012596 A ECSP13012596 A EC SP13012596A
Authority
EC
Ecuador
Prior art keywords
solid forms
elaboration process
compound
pirimidine derivatives
pirimidine
Prior art date
Application number
Other languages
English (en)
Inventor
Piotr Karpinski
Prasad Koteswara Kapa
Baoqing Gong
Dietmar Flubacher
John Vincent Calienni
Liladhar Murlidhar Waykole
La Cruz Marilyn De
Hui Liu
Pascal Michel
Rasmus Mose
Maria Caterina Testa
Original Assignee
Novartis Ag
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=44773179&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP13012596(A) "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 ECSP13012596A publication Critical patent/ECSP13012596A/es

Links

Classifications

    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyridine Compounds (AREA)

Abstract

La invención se refiere a procesos para la elaboración de un compuesto de la fórmula 5: o de un estereoisómero, tautómero o una sal del mismo, en donde los sustituyentes son como se definen en la memoria descriptiva. La invención se refiere además a nuevos procesos de elaboración para formas sólidas específicas del compuesto A y sus sales, a estas formas sólidas, y al uso de tales formas sólidas para el tratamiento terapéutico de animales de sangre caliente.
ECSP13012596 2010-10-01 2013-04-30 Proceso de elaboración para derivados de pirimidina ECSP13012596A (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
ECSP13012596A true ECSP13012596A (es) 2013-07-31

Family

ID=44773179

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13012596 ECSP13012596A (es) 2010-10-01 2013-04-30 Proceso de elaboración para derivados de pirimidina

Country Status (30)

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)
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 (2) PH12013500579A1 (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)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9271988B2 (en) 2011-07-01 2016-03-01 Novartis Ag Combination therapy comprising a CDK4/6 inhibitor and a P13K inhibitor for use in the treatment of cancer
MX342326B (es) 2011-09-27 2016-09-26 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
ES2605638T3 (es) * 2012-10-23 2017-03-15 Novartis Ag Proceso Mejorado para fabricar 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina
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
CA2903979A1 (en) 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant 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
CN106831722B (zh) * 2013-10-16 2019-08-30 上海璎黎药业有限公司 稠合杂环化合物、其制备方法、药物组合物和用途
BR112016023811B8 (pt) 2014-04-22 2023-01-10 Piqur Therapeutics Ag Método para fabricação para derivados de triazina, pirimidina e piridina, seus intermediários e seus métodos de fabricação
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
JP6397577B2 (ja) * 2014-12-17 2018-09-26 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. 2−モルホリノ−4,6−二置換ピリミジン誘導体、その製法および医薬における使用
US9481665B2 (en) * 2015-03-13 2016-11-01 Yong Xu Process for preparing PI3K inhibitor buparsilib
WO2016151501A1 (en) 2015-03-25 2016-09-29 Novartis Ag Pharmaceutical combinations
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
HRP20220227T1 (hr) * 2015-12-16 2022-04-29 Genentech, Inc. Postupak priprave tricikličnih spojeva inhibitora p13k i postupci upotrebe navedenih spojeva u liječenju raka
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6124476A (en) 1998-04-17 2000-09-26 Symyx Technologies, Inc. Catalyst ligands, catalyst compositions, catalyst metal complexes and processes for cross-coupling aromatic boron compounds with aromatic halogens or perfluoroalkylsulfonates
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
DK2316831T3 (da) 2002-11-21 2013-06-10 Novartis Ag 2-(Morpholin-4-yl)pyrimidiner som phosphotidylinositol (PI)-3-kinaseinhibitorer samt deres anvendelse ved behandling af cancer
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2008023159A1 (en) 2006-08-24 2008-02-28 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
CA2675558A1 (en) 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
CA2760179A1 (en) * 2009-05-15 2010-11-18 Novartis Ag Combination of a phosphoinositide 3-kinase inhibitor and an antidiabetic compound

Also Published As

Publication number Publication date
PH12015501585A1 (en) 2015-09-21
NZ608285A (en) 2014-06-27
AU2011308856B2 (en) 2015-04-23
KR20130119928A (ko) 2013-11-01
WO2012044727A2 (en) 2012-04-05
US9452994B2 (en) 2016-09-27
CN103140479B (zh) 2015-04-08
CO6700837A2 (es) 2013-06-28
PE20140002A1 (es) 2014-01-21
JP2013541536A (ja) 2013-11-14
PH12013500579A1 (en) 2016-06-10
IL233282A0 (en) 2014-08-31
US9181215B2 (en) 2015-11-10
HUE041326T2 (hu) 2019-05-28
TW201215605A (en) 2012-04-16
EP3040333A1 (en) 2016-07-06
EP3040333B1 (en) 2018-09-12
US9359326B2 (en) 2016-06-07
RU2013120326A (ru) 2014-11-20
JP5998145B2 (ja) 2016-09-28
HK1220686A1 (en) 2017-05-12
US20130225571A1 (en) 2013-08-29
AU2015200938B2 (en) 2015-11-19
AU2015200938A1 (en) 2015-03-12
AU2011308856A1 (en) 2013-03-28
LT3040333T (lt) 2018-12-10
MX2013003507A (es) 2013-05-20
MY160785A (en) 2017-03-15
WO2012044727A3 (en) 2012-06-07
BR112013007123B1 (pt) 2021-11-09
KR20180123586A (ko) 2018-11-16
CA2813333A1 (en) 2012-04-05
CA2813333C (en) 2019-01-15
PT3040333T (pt) 2018-12-04
AR083213A1 (es) 2013-02-06
GT201300080A (es) 2014-07-18
TWI540133B (zh) 2016-07-01
US20150232446A1 (en) 2015-08-20
CN104945373A (zh) 2015-09-30
AU2015200936A1 (en) 2015-03-12
RU2576619C2 (ru) 2016-03-10
DK3040333T3 (da) 2019-01-02
CL2013000850A1 (es) 2013-09-27
IL238046A (en) 2016-08-31
EP2621908A2 (en) 2013-08-07
CN103140479A (zh) 2013-06-05
AU2015246141B2 (en) 2016-07-07
SG188439A1 (en) 2013-05-31
CL2015001088A1 (es) 2015-07-10
SI3040333T1 (sl) 2019-01-31
RU2015150728A (ru) 2019-01-15
CN104987321A (zh) 2015-10-21
JP2016106091A (ja) 2016-06-16
AU2015246141A1 (en) 2015-11-12
ES2699951T3 (es) 2019-02-13
JP2016128414A (ja) 2016-07-14
IL233282A (en) 2016-08-31
PL3040333T3 (pl) 2019-03-29
BR112013007123A2 (pt) 2016-06-14
IL225113A (en) 2016-08-31
US20160251334A1 (en) 2016-09-01
MX354482B (es) 2018-03-07

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