ES2699951T3 - Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 - Google Patents

Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 Download PDF

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Publication number
ES2699951T3
ES2699951T3 ES16151719T ES16151719T ES2699951T3 ES 2699951 T3 ES2699951 T3 ES 2699951T3 ES 16151719 T ES16151719 T ES 16151719T ES 16151719 T ES16151719 T ES 16151719T ES 2699951 T3 ES2699951 T3 ES 2699951T3
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compound
polymorph
formula
ray powder
monohydrochloride
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ES16151719T
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English (en)
Spanish (es)
Inventor
John Vincent Calienni
La Cruz Marilyn De
Dietmar Flubacher
Baoqing Gong
Prasad Koteswara Kapa
Piotr H Karpinski
Hui Liu
Pascal Michel
Rasmus Mose
Maria Caterina Testa
Liladhar Murlidhar Waykole
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Novartis AG
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Novartis AG
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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 Table
    • 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 Table
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyridine Compounds (AREA)
ES16151719T 2010-10-01 2011-09-29 Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 Active ES2699951T3 (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
ES2699951T3 true ES2699951T3 (es) 2019-02-13

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ID=44773179

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ES16151719T Active ES2699951T3 (es) 2010-10-01 2011-09-29 Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3

Country Status (30)

Country Link
US (3) US9181215B2 (enExample)
EP (2) EP2621908A2 (enExample)
JP (3) JP5998145B2 (enExample)
KR (2) KR20130119928A (enExample)
CN (3) CN104987321A (enExample)
AR (1) AR083213A1 (enExample)
AU (4) AU2011308856B2 (enExample)
BR (1) BR112013007123B1 (enExample)
CA (1) CA2813333C (enExample)
CL (2) CL2013000850A1 (enExample)
CO (1) CO6700837A2 (enExample)
DK (1) DK3040333T3 (enExample)
EC (1) ECSP13012596A (enExample)
ES (1) ES2699951T3 (enExample)
GT (1) GT201300080A (enExample)
HU (1) HUE041326T2 (enExample)
IL (3) IL225113A (enExample)
LT (1) LT3040333T (enExample)
MX (1) MX354482B (enExample)
MY (1) MY160785A (enExample)
NZ (1) NZ608285A (enExample)
PE (1) PE20140002A1 (enExample)
PH (2) PH12013500579A1 (enExample)
PL (1) PL3040333T3 (enExample)
PT (1) PT3040333T (enExample)
RU (2) RU2015150728A (enExample)
SG (1) SG188439A1 (enExample)
SI (1) SI3040333T1 (enExample)
TW (1) TWI540133B (enExample)
WO (1) WO2012044727A2 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20140040770A (ko) 2011-07-01 2014-04-03 노파르티스 아게 암 치료에 사용하기 위한 cdk4/6 억제제 및 pi3k 억제제를 포함하는 조합 요법
PH12014500682A1 (en) 2011-09-27 2014-05-12 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
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
WO2014141104A1 (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
RU2663999C2 (ru) * 2013-10-16 2018-08-14 Шанхай Инли Фармасьютикал Ко., Лтд Конденсированное гетероциклическое соединение, способ его получения, его фармацевтическая композиция и применения
RU2688665C2 (ru) * 2014-04-22 2019-05-22 Университет Базель Новый способ получения производных триазина, пиримидина и пиридина
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
CN107001348B (zh) * 2014-12-17 2019-10-11 上海海雁医药科技有限公司 2-吗啉-4,6-二取代的嘧啶衍生物、其制法与医药上的用途
US9481665B2 (en) * 2015-03-13 2016-11-01 Yong Xu Process for preparing PI3K inhibitor buparsilib
EP3273959A1 (en) 2015-03-25 2018-01-31 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
PL3978500T3 (pl) * 2015-12-16 2024-03-11 Genentech, Inc. Sposób wytwarzania tricyklicznych związków inhibitorów pi3k
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)

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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
CA2507100C (en) 2002-11-21 2012-10-09 Chiron Corporation 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
EP2057140B1 (en) 2006-08-24 2012-08-08 AstraZeneca AB Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
MX2009008341A (es) * 2007-02-06 2009-08-12 Novartis Ag Inhibidores de cinasa de pi3 y metodos para su uso.
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
JP2012526772A (ja) * 2009-05-15 2012-11-01 ノバルティス アーゲー ホスホイノシチド3−キナーゼ阻害剤および抗糖尿病性化合物の組合せ剤

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HK1220686A1 (en) 2017-05-12
MY160785A (en) 2017-03-15
MX2013003507A (es) 2013-05-20
US20130225571A1 (en) 2013-08-29
US20160251334A1 (en) 2016-09-01
WO2012044727A2 (en) 2012-04-05
JP2013541536A (ja) 2013-11-14
US20150232446A1 (en) 2015-08-20
BR112013007123A2 (pt) 2016-06-14
KR20180123586A (ko) 2018-11-16
IL233282A0 (en) 2014-08-31
CA2813333A1 (en) 2012-04-05
PT3040333T (pt) 2018-12-04
IL225113A (en) 2016-08-31
CO6700837A2 (es) 2013-06-28
JP2016128414A (ja) 2016-07-14
CL2015001088A1 (es) 2015-07-10
ECSP13012596A (es) 2013-07-31
US9359326B2 (en) 2016-06-07
WO2012044727A3 (en) 2012-06-07
AU2011308856A1 (en) 2013-03-28
IL238046A (en) 2016-08-31
EP3040333A1 (en) 2016-07-06
CN103140479A (zh) 2013-06-05
AU2015246141A1 (en) 2015-11-12
NZ608285A (en) 2014-06-27
TW201215605A (en) 2012-04-16
GT201300080A (es) 2014-07-18
MX354482B (es) 2018-03-07
CA2813333C (en) 2019-01-15
RU2013120326A (ru) 2014-11-20
JP5998145B2 (ja) 2016-09-28
AR083213A1 (es) 2013-02-06
PH12015501585A1 (en) 2015-09-21
HUE041326T2 (hu) 2019-05-28
CN104945373A (zh) 2015-09-30
AU2015246141B2 (en) 2016-07-07
JP2016106091A (ja) 2016-06-16
AU2011308856B2 (en) 2015-04-23
PH12013500579A1 (en) 2016-06-10
RU2015150728A (ru) 2019-01-15
KR20130119928A (ko) 2013-11-01
PL3040333T3 (pl) 2019-03-29
AU2015200938A1 (en) 2015-03-12
TWI540133B (zh) 2016-07-01
CL2013000850A1 (es) 2013-09-27
CN104987321A (zh) 2015-10-21
US9452994B2 (en) 2016-09-27
RU2576619C2 (ru) 2016-03-10
SI3040333T1 (sl) 2019-01-31
AU2015200938B2 (en) 2015-11-19
CN103140479B (zh) 2015-04-08
LT3040333T (lt) 2018-12-10
EP2621908A2 (en) 2013-08-07
SG188439A1 (en) 2013-05-31
BR112013007123B1 (pt) 2021-11-09
US9181215B2 (en) 2015-11-10
AU2015200936A1 (en) 2015-03-12
PE20140002A1 (es) 2014-01-21
IL233282A (en) 2016-08-31
EP3040333B1 (en) 2018-09-12
DK3040333T3 (da) 2019-01-02

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