AU2011308856B2 - Manufacturing process for pyrimidine derivatives - Google Patents

Manufacturing process for pyrimidine derivatives Download PDF

Info

Publication number
AU2011308856B2
AU2011308856B2 AU2011308856A AU2011308856A AU2011308856B2 AU 2011308856 B2 AU2011308856 B2 AU 2011308856B2 AU 2011308856 A AU2011308856 A AU 2011308856A AU 2011308856 A AU2011308856 A AU 2011308856A AU 2011308856 B2 AU2011308856 B2 AU 2011308856B2
Authority
AU
Australia
Prior art keywords
compound
formula
substituted
unsubstituted
polymorph form
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
AU2011308856A
Other languages
English (en)
Other versions
AU2011308856A1 (en
Inventor
John Vincent Calienni
Marilyn De La Cruz
Dietmar Flubacher
Baoqing Gong
Prasad Koteswara Kapa
Piotr H. Karpinski
Hui Liu
Pascal Michel
Rasmus Mose
Maria Caterina Testa
Liladhar Murlidhar Waykole
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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=AU2011308856(B2) "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 AU2011308856A1 publication Critical patent/AU2011308856A1/en
Priority to AU2015200938A priority Critical patent/AU2015200938B2/en
Priority to AU2015200936A priority patent/AU2015200936A1/en
Application granted granted Critical
Publication of AU2011308856B2 publication Critical patent/AU2011308856B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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)
  • 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)
AU2011308856A 2010-10-01 2011-09-29 Manufacturing process for pyrimidine derivatives Active AU2011308856B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2015200938A AU2015200938B2 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives
AU2015200936A AU2015200936A1 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US38872110P 2010-10-01 2010-10-01
US61/388,721 2010-10-01
US201161494915P 2011-06-09 2011-06-09
US61/494,915 2011-06-09
PCT/US2011/053808 WO2012044727A2 (en) 2010-10-01 2011-09-29 Manufacturing process for pyrimidine derivatives

Related Child Applications (2)

Application Number Title Priority Date Filing Date
AU2015200938A Division AU2015200938B2 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives
AU2015200936A Division AU2015200936A1 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives

Publications (2)

Publication Number Publication Date
AU2011308856A1 AU2011308856A1 (en) 2013-03-28
AU2011308856B2 true AU2011308856B2 (en) 2015-04-23

Family

ID=44773179

Family Applications (4)

Application Number Title Priority Date Filing Date
AU2011308856A Active AU2011308856B2 (en) 2010-10-01 2011-09-29 Manufacturing process for pyrimidine derivatives
AU2015200936A Abandoned AU2015200936A1 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives
AU2015200938A Ceased AU2015200938B2 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives
AU2015246141A Ceased AU2015246141B2 (en) 2010-10-01 2015-10-23 Manufacturing process for pyrimidine derivatives

Family Applications After (3)

Application Number Title Priority Date Filing Date
AU2015200936A Abandoned AU2015200936A1 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives
AU2015200938A Ceased AU2015200938B2 (en) 2010-10-01 2015-02-24 Manufacturing process for pyrimidine derivatives
AU2015246141A Ceased AU2015246141B2 (en) 2010-10-01 2015-10-23 Manufacturing process for pyrimidine derivatives

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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007084786A1 (en) * 2006-01-20 2007-07-26 Novartis Ag Pyrimidine derivatives used as pi-3 kinase inhibitors
AU2010247397A1 (en) * 2009-05-15 2011-11-03 Novartis Ag Combination of a phosphoinositide 3-kinase inhibitor and an antidiabetic compound

Family Cites Families (6)

* 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
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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007084786A1 (en) * 2006-01-20 2007-07-26 Novartis Ag Pyrimidine derivatives used as pi-3 kinase inhibitors
AU2010247397A1 (en) * 2009-05-15 2011-11-03 Novartis Ag Combination of a phosphoinositide 3-kinase inhibitor and an antidiabetic compound

Also Published As

Publication number Publication date
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
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
ES2699951T3 (es) 2019-02-13
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

Similar Documents

Publication Publication Date Title
AU2011308856B2 (en) Manufacturing process for pyrimidine derivatives
AU2003295776B2 (en) 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
US20170174687A1 (en) FUSED QUINOLINE COMPUNDS AS PI3K, mTOR INHIBITORS
CN1735607B (zh) 2,4,6-三取代的嘧啶作为磷脂酰肌醇(pi)3-激酶抑制剂及其在治疗癌症中的应用
HK1220686B (en) Crystalline forms of 5-(2,6-di-4-morpholinyl-4-pyridmidinyl)-4-trifluoromethylpyridin-2-amine, a pik3 inhibitor

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)