MA40895B1 - Synthèse de copanlisib et son sel de dichlorhydrate - Google Patents

Synthèse de copanlisib et son sel de dichlorhydrate

Info

Publication number
MA40895B1
MA40895B1 MA40895A MA40895A MA40895B1 MA 40895 B1 MA40895 B1 MA 40895B1 MA 40895 A MA40895 A MA 40895A MA 40895 A MA40895 A MA 40895A MA 40895 B1 MA40895 B1 MA 40895B1
Authority
MA
Morocco
Prior art keywords
copanlisib
copanisib
dihydrochloride
synthesis
dihydrochloride salt
Prior art date
Application number
MA40895A
Other languages
English (en)
Other versions
MA40895A (fr
Inventor
Franz-Josef Mais
Jan-Georg Peters
Philipp Rubenbauer
Daniel Götz
Danja Grossbach
Heiko Schirmer
Juergen Stiehl
Kai Lovis
Andreas Lender
Martin Seyfried
Theodor Zweifel
Maurus Marty
Günter Weingärtner
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 MA40895A publication Critical patent/MA40895A/fr
Publication of MA40895B1 publication Critical patent/MA40895B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/08—Heterocyclic 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
    • C07D295/084—Heterocyclic 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
    • C07D295/088—Heterocyclic 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne un nouveau procédé de préparation du copanlisib, du dihydrochlorure de copanlisib ou d'hydrates de dihydrochlorure de copanlisib et de nouveaux composés intermédiaires, ainsi que l'utilisation de ces nouveaux composés intermédiaires pour la préparation dudit copanlisib, dudit dihydrochlorure de copanlisib ou desdits hydrates de dihydrochlorure de copanlisib. La présente invention concerne également des hydrates de dihydrochlorure de copanlisib en tant que composés chimiques.
MA40895A 2014-11-07 2015-11-05 Synthèse de copanlisib et son sel de dichlorhydrate MA40895B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14192203.9A EP3018127A1 (fr) 2014-11-07 2014-11-07 Synthèse de copanlisib et son sel de dichlorhydrate
PCT/EP2015/075789 WO2016071435A2 (fr) 2014-11-07 2015-11-05 Synthèse du copanlisib et de son dihydrochlorure

Publications (2)

Publication Number Publication Date
MA40895A MA40895A (fr) 2017-09-13
MA40895B1 true MA40895B1 (fr) 2019-07-31

Family

ID=51866061

Family Applications (1)

Application Number Title Priority Date Filing Date
MA40895A MA40895B1 (fr) 2014-11-07 2015-11-05 Synthèse de copanlisib et son sel de dichlorhydrate

Country Status (47)

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

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2168583A1 (fr) 2008-09-24 2010-03-31 Bayer Schering Pharma Aktiengesellschaft Utilisation de 2,3-dihydroimidazo[1,2-c]quinazolines substituées pour le traitement du myélome
EP2508525A1 (fr) 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Sels de 2,3-dihydroimidazo[1,2-C]quinazoline substitutés
MX2015014171A (es) 2013-04-08 2015-12-16 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas.
JP6867295B2 (ja) 2015-03-09 2021-04-28 バイエル ファーマ アクチエンゲゼルシャフト 置換２，３−ジヒドロイミダゾ［１，２−ｃ］キナゾリンを含んでいる組合せ
EP3426657B1 (fr) 2016-03-08 2022-07-13 Bayer Pharma Aktiengesellschaft 2-amino-n-[7-méthoxy-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamides
JP2019532922A (ja) 2016-09-23 2019-11-14 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
WO2018215282A1 (fr) 2017-05-26 2018-11-29 Bayer Pharma Aktiengesellschaft Combinaison d'inhibiteurs de bub1 et de pi3k
CA3068324A1 (fr) 2017-06-28 2019-01-03 Bayer Consumer Care Ag Combinaison d'un inhibiteur de pi3k et d'un antagoniste du recepteur des androgenes
EP3498266A1 (fr) 2017-12-15 2019-06-19 Bayer Consumer Care AG Formulations de copanlisib
IL272857B2 (en) 2017-09-08 2024-03-01 Bayer Consumer Care Ag Cofanalisib formulations
WO2023139125A1 (fr) 2022-01-18 2023-07-27 Synthon B.V. Procédé amélioré de préparation de copanlisib
WO2023218032A1 (fr) 2022-05-13 2023-11-16 Synthon B.V. Formes solides de sels de copanlisib

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2003016304A1 (fr) * 2001-08-15 2003-02-27 E. I. Du Pont De Nemours And Company Amides aryle ortho-heterocycliques substitues permettant de lutter contre des ravageurs invertebres
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
JP5620275B2 (ja) * 2008-01-14 2014-11-05 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 超増殖性疾患及び脈管形成に関連する疾病を処理するために有用なスルホン置換された２，３−ジヒドロイミダゾ［１，２−ｃ］キナゾリン誘導体類
EP2168583A1 (fr) 2008-09-24 2010-03-31 Bayer Schering Pharma Aktiengesellschaft Utilisation de 2,3-dihydroimidazo[1,2-c]quinazolines substituées pour le traitement du myélome
JO3733B1 (ar) 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
EP2508525A1 (fr) * 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Sels de 2,3-dihydroimidazo[1,2-C]quinazoline substitutés
MX2015014171A (es) 2013-04-08 2015-12-16 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas.
EP3077002B1 (fr) 2013-12-03 2020-04-22 Bayer Pharma Aktiengesellschaft Combinaisons d'inhibiteurs de pi3k
EP3018131A1 (fr) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthèse de copanlisib et son sel de dichlorhydrate
MX2017011607A (es) 2015-03-09 2018-04-10 Bayer Pharma AG Uso de 2,3-dihidroimidazol[1,2-c]quinazolinas sustituidas.
JP6867295B2 (ja) 2015-03-09 2021-04-28 バイエル ファーマ アクチエンゲゼルシャフト 置換２，３−ジヒドロイミダゾ［１，２−ｃ］キナゾリンを含んでいる組合せ
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
MA43957A (fr) 2016-02-01 2018-12-12 Bayer Pharma AG Biomarqueurs de copanlisib
EP3426657B1 (fr) 2016-03-08 2022-07-13 Bayer Pharma Aktiengesellschaft 2-amino-n-[7-méthoxy-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamides
JP2019532922A (ja) 2016-09-23 2019-11-14 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

Also Published As

Publication number Publication date
ZA201703867B (en) 2019-07-31
DK3215493T3 (da) 2019-05-06
PL3215493T3 (pl) 2019-07-31
AR102570A1 (es) 2017-03-08
WO2016071435A3 (fr) 2016-06-30
ME03358B (fr) 2019-10-20
BR112017009470B1 (pt) 2022-11-01
CR20170184A (es) 2017-06-20
ECSP17027755A (es) 2017-06-30
BR112017009470A2 (pt) 2018-01-02
DOP2017000112A (es) 2017-06-15
SG11201703702RA (en) 2017-06-29
CA2966800C (fr) 2023-02-21
TWI697495B (zh) 2020-07-01
EA201790983A1 (ru) 2017-10-31
TR201905217T4 (tr) 2019-05-21
JP6691115B2 (ja) 2020-04-28
JO3644B1 (ar) 2020-08-27
TN2017000179A1 (en) 2018-10-19
ES2721778T3 (es) 2019-08-05
NI201700054A (es) 2017-07-17
TW201625634A (zh) 2016-07-16
US20180282337A1 (en) 2018-10-04
LT3215493T (lt) 2019-04-25
CO2017004532A2 (es) 2017-07-19
HUE042866T2 (hu) 2019-07-29
PE20170897A1 (es) 2017-07-12
RS58579B1 (sr) 2019-05-31
SA517381462B1 (ar) 2021-01-25
CU20170061A7 (es) 2017-10-05
HRP20190720T1 (hr) 2019-06-14
UA122398C2 (uk) 2020-11-10
CU24489B1 (es) 2020-12-17
PT3215493T (pt) 2019-05-21
US10494372B2 (en) 2019-12-03
CN107278204A (zh) 2017-10-20
JP2017534631A (ja) 2017-11-24
EP3215493A2 (fr) 2017-09-13
CA2966800A1 (fr) 2016-05-12
NZ731287A (en) 2023-01-27
CL2017001131A1 (es) 2018-01-19
SI3215493T1 (sl) 2019-05-31
HK1245774A1 (zh) 2018-08-31
AU2015341788B2 (en) 2020-01-16
UY36392A (es) 2016-06-30
IL251874A0 (en) 2017-06-29
MX2017005893A (es) 2017-06-30
AU2015341788A1 (en) 2017-05-18
KR20170082563A (ko) 2017-07-14
EA035558B1 (ru) 2020-07-07
SV2017005433A (es) 2018-04-30
MY189852A (en) 2022-03-14
WO2016071435A2 (fr) 2016-05-12
KR102566834B1 (ko) 2023-08-16
MX366904B (es) 2019-07-30
MA40895A (fr) 2017-09-13
EP3018127A1 (fr) 2016-05-11
EP3215493B1 (fr) 2019-01-23
CN107278204B (zh) 2019-12-17
CY1121602T1 (el) 2020-05-29
PH12017500833A1 (en) 2017-10-18

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