SV2017005433A - Síntesis de copanlisib y su sal diclorhidrato - Google Patents

Síntesis de copanlisib y su sal diclorhidrato

Info

Publication number
SV2017005433A
SV2017005433A SV2017005433A SV2017005433A SV2017005433A SV 2017005433 A SV2017005433 A SV 2017005433A SV 2017005433 A SV2017005433 A SV 2017005433A SV 2017005433 A SV2017005433 A SV 2017005433A SV 2017005433 A SV2017005433 A SV 2017005433A
Authority
SV
El Salvador
Prior art keywords
copanlisib
diclorhydrate
synthesis
salt
new
Prior art date
Application number
SV2017005433A
Other languages
English (en)
Inventor
Jan-Georg Peters
Philipp Rubenbauer
Daniel Götz
Danja Groβbach
Franz-Josef Mais
Heiko Schirmer
Maurus Marty
Juergen Stiehl
Kai Lovis
Martin Deyfried
Theodor Zweifel
Günter Weingärtner
Andreas Lender
Original Assignee
Bayer Pharma 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
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of SV2017005433A publication Critical patent/SV2017005433A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/22Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/24Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

LA PRESENTE INVENCIÓN SE RELACIONA CON UN NUEVO MÉTODO PARA PREPARAR COPANLISIB, DICLORHIDRATO DE COPANLISIB, O HIDRATOS DE DICLORHIDRATO DE COPANLISIB, CON NUEVOS COMPUESTOS INTERMEDIARIOS, Y CON EL USO DE DICHOS NUEVOS COMPUESTOS INTERMEDIARIOS EN LA PREPARACIÓN DE COPANLISIB, DICLORHIDRATO DE COPANLISIB, O HIDRATOS DE DICLORHIDRATO DE COPANLISIB. LA PRESENTE INVENCIÓN TAMBIÉN SE RELACIONA CON HIDRATOS DE DICLORHIDRATO DE COPANLISIB COMO COMPUESTOS.
SV2017005433A 2014-11-07 2017-05-05 Síntesis de copanlisib y su sal diclorhidrato SV2017005433A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14192203.9A EP3018127A1 (en) 2014-11-07 2014-11-07 Synthesis of copanlisib and its dihydrochloride salt

Publications (1)

Publication Number Publication Date
SV2017005433A true SV2017005433A (es) 2018-04-30

Family

ID=51866061

Family Applications (1)

Application Number Title Priority Date Filing Date
SV2017005433A SV2017005433A (es) 2014-11-07 2017-05-05 Síntesis de copanlisib y su sal diclorhidrato

Country Status (47)

Country Link
US (1) US10494372B2 (es)
EP (2) EP3018127A1 (es)
JP (1) JP6691115B2 (es)
KR (1) KR102566834B1 (es)
CN (1) CN107278204B (es)
AR (1) AR102570A1 (es)
AU (1) AU2015341788B2 (es)
BR (1) BR112017009470B1 (es)
CA (1) CA2966800C (es)
CL (1) CL2017001131A1 (es)
CO (1) CO2017004532A2 (es)
CR (1) CR20170184A (es)
CU (1) CU24489B1 (es)
CY (1) CY1121602T1 (es)
DK (1) DK3215493T3 (es)
DO (1) DOP2017000112A (es)
EA (1) EA035558B1 (es)
EC (1) ECSP17027755A (es)
ES (1) ES2721778T3 (es)
HK (1) HK1245774A1 (es)
HR (1) HRP20190720T1 (es)
HU (1) HUE042866T2 (es)
IL (1) IL251874A0 (es)
JO (1) JO3644B1 (es)
LT (1) LT3215493T (es)
MA (1) MA40895B1 (es)
ME (1) ME03358B (es)
MX (1) MX366904B (es)
MY (1) MY189852A (es)
NI (1) NI201700054A (es)
NZ (1) NZ731287A (es)
PE (1) PE20170897A1 (es)
PH (1) PH12017500833A1 (es)
PL (1) PL3215493T3 (es)
PT (1) PT3215493T (es)
RS (1) RS58579B1 (es)
SA (1) SA517381462B1 (es)
SG (1) SG11201703702RA (es)
SI (1) SI3215493T1 (es)
SV (1) SV2017005433A (es)
TN (1) TN2017000179A1 (es)
TR (1) TR201905217T4 (es)
TW (1) TWI697495B (es)
UA (1) UA122398C2 (es)
UY (1) UY36392A (es)
WO (1) WO2016071435A2 (es)
ZA (1) ZA201703867B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2168583A1 (en) 2008-09-24 2010-03-31 Bayer Schering Pharma Aktiengesellschaft Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma
EP2508525A1 (en) 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts
UA119537C2 (uk) 2013-04-08 2019-07-10 Байєр Фарма Акцієнгезелльшафт ЗАСТОСУВАННЯ ЗАМІЩЕНИХ 2,3-ДИГІДРОІМІДАЗО[1,2-c]ХІНАЗОЛІНІВ ДЛЯ ЛІКУВАННЯ ЛІМФОМ
CA2978830A1 (en) 2015-03-09 2016-09-15 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations
EP3426657B1 (en) 2016-03-08 2022-07-13 Bayer Pharma Aktiengesellschaft 2 amino n [7 methoxy 2, 3-dihydroimidazo-[1, 2-c]quinazolin-5-yl]pyrimidine 5 carboxamides
CA3037626A1 (en) 2016-09-23 2018-03-29 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors
WO2018215282A1 (en) 2017-05-26 2018-11-29 Bayer Pharma Aktiengesellschaft Combination of bub1 and pi3k inhibitors
WO2019002068A1 (en) 2017-06-28 2019-01-03 Bayer Consumer Care Ag COMBINATION OF A PI3K INHIBITOR AND AN ANDROGEN RECEPTOR ANTAGONIST
EP3498266A1 (en) 2017-12-15 2019-06-19 Bayer Consumer Care AG Formulations of copanlisib
JP2020533292A (ja) 2017-09-08 2020-11-19 バイエル・コンシューマー・ケア・アクチェンゲゼルシャフトBayer Consumer Care AG コパンリシブの製剤
WO2023139125A1 (en) 2022-01-18 2023-07-27 Synthon B.V. Improved process for preparation of copanlisib
WO2023218032A1 (en) 2022-05-13 2023-11-16 Synthon B.V. Solid forms of copanlisib salts

Family Cites Families (20)

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US1003580A (en) 1910-08-10 1911-09-19 Remington Typewriter Co Type-writing machine.
US6221877B1 (en) * 2000-04-12 2001-04-24 Regents Of The University Of California Substituted 4-phthalimidocarboxanilides as inhibitors of purine salvage phosphoribosyltransferases
IT1319674B1 (it) * 2000-12-01 2003-10-23 Erregierre Spa Processo per la preparazione dell'acido1-(aminometil)cicloesanacetico.
TW565582B (en) * 2001-04-13 2003-12-11 Kaneka Corp Diamine, acid dianhydride, and reactive group containing polyimide composition prepared therefrom and preparing them
EP1417204B1 (en) * 2001-08-15 2006-01-18 E. I. du Pont de Nemours and Company Ortho-heterocyclic substituted aryl amides for controlling invertebrate pests
SI1549652T1 (sl) 2002-09-30 2009-04-30 Bayer Healthcare Ag Kondenzirani azolpirimidinski derivati
AR064106A1 (es) 2006-12-05 2009-03-11 Bayer Schering Pharma Ag Derivados de 2,3-dihidroimidazo [1,2-c] quinazolina sustituida utiles para el tratamiento de enfermedades y trastornos hiper-proliferativos asociados con la angiogenesis
US8859572B2 (en) 2008-01-14 2014-10-14 Bayer Intellectual Property Gmbh Sulfone substituted 2,3-dihydroimidazo [1,2-C] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis
EP2168583A1 (en) 2008-09-24 2010-03-31 Bayer Schering Pharma Aktiengesellschaft Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma
JO3733B1 (ar) 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
EP2508525A1 (en) 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts
UA119537C2 (uk) 2013-04-08 2019-07-10 Байєр Фарма Акцієнгезелльшафт ЗАСТОСУВАННЯ ЗАМІЩЕНИХ 2,3-ДИГІДРОІМІДАЗО[1,2-c]ХІНАЗОЛІНІВ ДЛЯ ЛІКУВАННЯ ЛІМФОМ
JP6499657B2 (ja) 2013-12-03 2019-04-10 バイエル ファーマ アクチエンゲゼルシャフト Pi3k阻害剤の組み合わせ
EP3018131A1 (en) * 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
CA2978830A1 (en) 2015-03-09 2016-09-15 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations
EP3268005A1 (en) 2015-03-09 2018-01-17 Bayer Pharma Aktiengesellschaft Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines
TN2018000271A1 (en) 2016-02-01 2020-01-16 Bayer Pharma AG Copanlisib biomarkers.
JP2019512003A (ja) 2016-02-01 2019-05-09 バイエル ファーマ アクチエンゲゼルシャフト コパンリシブバイオマーカー
EP3426657B1 (en) 2016-03-08 2022-07-13 Bayer Pharma Aktiengesellschaft 2 amino n [7 methoxy 2, 3-dihydroimidazo-[1, 2-c]quinazolin-5-yl]pyrimidine 5 carboxamides
CA3037626A1 (en) 2016-09-23 2018-03-29 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors

Also Published As

Publication number Publication date
NI201700054A (es) 2017-07-17
ZA201703867B (en) 2019-07-31
TN2017000179A1 (en) 2018-10-19
ECSP17027755A (es) 2017-06-30
JO3644B1 (ar) 2020-08-27
MX366904B (es) 2019-07-30
MX2017005893A (es) 2017-06-30
SI3215493T1 (sl) 2019-05-31
SG11201703702RA (en) 2017-06-29
HK1245774A1 (zh) 2018-08-31
WO2016071435A3 (en) 2016-06-30
PT3215493T (pt) 2019-05-21
CY1121602T1 (el) 2020-05-29
PH12017500833A1 (en) 2017-10-18
CN107278204A (zh) 2017-10-20
LT3215493T (lt) 2019-04-25
CA2966800C (en) 2023-02-21
UY36392A (es) 2016-06-30
EP3215493A2 (en) 2017-09-13
AU2015341788B2 (en) 2020-01-16
KR102566834B1 (ko) 2023-08-16
DK3215493T3 (da) 2019-05-06
CO2017004532A2 (es) 2017-07-19
PL3215493T3 (pl) 2019-07-31
TWI697495B (zh) 2020-07-01
NZ731287A (en) 2023-01-27
AU2015341788A1 (en) 2017-05-18
EP3215493B1 (en) 2019-01-23
WO2016071435A2 (en) 2016-05-12
ES2721778T3 (es) 2019-08-05
CL2017001131A1 (es) 2018-01-19
MA40895B1 (fr) 2019-07-31
TW201625634A (zh) 2016-07-16
TR201905217T4 (tr) 2019-05-21
HUE042866T2 (hu) 2019-07-29
BR112017009470B1 (pt) 2022-11-01
CA2966800A1 (en) 2016-05-12
CU20170061A7 (es) 2017-10-05
HRP20190720T1 (hr) 2019-06-14
RS58579B1 (sr) 2019-05-31
ME03358B (me) 2019-10-20
EP3018127A1 (en) 2016-05-11
CN107278204B (zh) 2019-12-17
IL251874A0 (en) 2017-06-29
JP6691115B2 (ja) 2020-04-28
SA517381462B1 (ar) 2021-01-25
JP2017534631A (ja) 2017-11-24
CR20170184A (es) 2017-06-20
EA201790983A1 (ru) 2017-10-31
PE20170897A1 (es) 2017-07-12
MY189852A (en) 2022-03-14
KR20170082563A (ko) 2017-07-14
EA035558B1 (ru) 2020-07-07
CU24489B1 (es) 2020-12-17
UA122398C2 (uk) 2020-11-10
AR102570A1 (es) 2017-03-08
BR112017009470A2 (pt) 2018-01-02
DOP2017000112A (es) 2017-06-15
US20180282337A1 (en) 2018-10-04
MA40895A (fr) 2017-09-13
US10494372B2 (en) 2019-12-03

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