TR201905217T4 - Kopanlisib ve bunun dihidroklorid tuzunun sentezi. - Google Patents

Kopanlisib ve bunun dihidroklorid tuzunun sentezi. Download PDF

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Publication number
TR201905217T4
TR201905217T4 TR2019/05217T TR201905217T TR201905217T4 TR 201905217 T4 TR201905217 T4 TR 201905217T4 TR 2019/05217 T TR2019/05217 T TR 2019/05217T TR 201905217 T TR201905217 T TR 201905217T TR 201905217 T4 TR201905217 T4 TR 201905217T4
Authority
TR
Turkey
Prior art keywords
kopanlisib
dihydrochloride
synthesis
dihydrochloride salt
copanlisib
Prior art date
Application number
TR2019/05217T
Other languages
English (en)
Inventor
Peters Jan-Georg
Rubenbauer Philipp
Gotz Daniel
Grossbach Danja
Mais Franz-Josef
Schirmer Heiko
Stiehl Juergen
Lovis Kai
Lender Andreas
Seyfried Martin
Zweifel Theodor
Marty Maurus
Weingärtner Gunter
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 TR201905217T4 publication Critical patent/TR201905217T4/tr

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    • 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

Abstract

Mevcut buluş, kopanlisib, kopanlisib dihidroklorid veya kopanlisib dihidroklorid hidratlarının hazırlanmasına yönelik yeni bir yöntem ile, yeni ara bileşikler ile ve söz konusu kopanlisib, kopanlisib dihidroklorid veya kopanlisib dihidroklorid hidratlarının hazırlanmasına yönelik söz konusu yeni ara bileşiklerin kullanımı ile ilgilidir. Mevcut buluş ayrıca bileşikler olarak kopanlisib dihidroklorid hidratları ile ilgilidir.
TR2019/05217T 2014-11-07 2015-11-05 Kopanlisib ve bunun dihidroklorid tuzunun sentezi. TR201905217T4 (tr)

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
TR201905217T4 true TR201905217T4 (tr) 2019-05-21

Family

ID=51866061

Family Applications (1)

Application Number Title Priority Date Filing Date
TR2019/05217T TR201905217T4 (tr) 2014-11-07 2015-11-05 Kopanlisib ve bunun dihidroklorid tuzunun sentezi.

Country Status (47)

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

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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
JP6368353B2 (ja) 2013-04-08 2018-08-01 バイエル ファーマ アクチエンゲゼルシャフト 置換された2,3−ジヒドロイミダゾ[1,2−c]キナゾリン類のリンパ腫治療への使用
AU2016231259A1 (en) 2015-03-09 2017-09-21 Bayer Healthcare Pharmaceuticals Inc. Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations
US10844066B2 (en) 2016-03-08 2020-11-24 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
EP3645005A1 (en) 2017-06-28 2020-05-06 Bayer Consumer Care AG Combination of a pi3k-inhibitor with an androgen receptor antagonist
TWI794288B (zh) 2017-09-08 2023-03-01 德商拜耳製藥公司 科帕利普(copanlisib)調配物
EP3498266A1 (en) 2017-12-15 2019-06-19 Bayer Consumer Care AG Formulations of copanlisib
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

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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
JO3733B1 (ar) 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
JP6368353B2 (ja) 2013-04-08 2018-08-01 バイエル ファーマ アクチエンゲゼルシャフト 置換された2,3−ジヒドロイミダゾ[1,2−c]キナゾリン類のリンパ腫治療への使用
US10117874B2 (en) 2013-12-03 2018-11-06 Bayer Pharma Aktiengesellschaft Combination of PI3K-inhibitors
EP3018131A1 (en) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
KR20180013850A (ko) 2015-03-09 2018-02-07 바이엘 파마 악티엔게젤샤프트 치환된 2,3-디히드로이미다조[1,2-c]퀴나졸린의 용도
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US10844066B2 (en) 2016-03-08 2020-11-24 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
ME03358B (me) 2019-10-20
CO2017004532A2 (es) 2017-07-19
JP2017534631A (ja) 2017-11-24
SI3215493T1 (sl) 2019-05-31
CY1121602T1 (el) 2020-05-29
CU20170061A7 (es) 2017-10-05
HRP20190720T1 (hr) 2019-06-14
JP6691115B2 (ja) 2020-04-28
CU24489B1 (es) 2020-12-17
UY36392A (es) 2016-06-30
TN2017000179A1 (en) 2018-10-19
KR20170082563A (ko) 2017-07-14
TWI697495B (zh) 2020-07-01
JO3644B1 (ar) 2020-08-27
RS58579B1 (sr) 2019-05-31
NI201700054A (es) 2017-07-17
WO2016071435A3 (en) 2016-06-30
EP3018127A1 (en) 2016-05-11
AU2015341788A1 (en) 2017-05-18
CR20170184A (es) 2017-06-20
US20180282337A1 (en) 2018-10-04
EP3215493A2 (en) 2017-09-13
ES2721778T3 (es) 2019-08-05
ZA201703867B (en) 2019-07-31
EA035558B1 (ru) 2020-07-07
HK1245774A1 (zh) 2018-08-31
DK3215493T3 (da) 2019-05-06
UA122398C2 (uk) 2020-11-10
MA40895B1 (fr) 2019-07-31
PT3215493T (pt) 2019-05-21
AU2015341788B2 (en) 2020-01-16
EP3215493B1 (en) 2019-01-23
BR112017009470A2 (pt) 2018-01-02
DOP2017000112A (es) 2017-06-15
MX2017005893A (es) 2017-06-30
BR112017009470B1 (pt) 2022-11-01
EA201790983A1 (ru) 2017-10-31
SA517381462B1 (ar) 2021-01-25
AR102570A1 (es) 2017-03-08
CL2017001131A1 (es) 2018-01-19
CN107278204B (zh) 2019-12-17
MA40895A (fr) 2017-09-13
MX366904B (es) 2019-07-30
NZ731287A (en) 2023-01-27
ECSP17027755A (es) 2017-06-30
CN107278204A (zh) 2017-10-20
US10494372B2 (en) 2019-12-03
TW201625634A (zh) 2016-07-16
WO2016071435A2 (en) 2016-05-12
IL251874A0 (en) 2017-06-29
HUE042866T2 (hu) 2019-07-29
PH12017500833A1 (en) 2017-10-18
CA2966800C (en) 2023-02-21
MY189852A (en) 2022-03-14
PL3215493T3 (pl) 2019-07-31
SV2017005433A (es) 2018-04-30
LT3215493T (lt) 2019-04-25
PE20170897A1 (es) 2017-07-12
KR102566834B1 (ko) 2023-08-16
SG11201703702RA (en) 2017-06-29
CA2966800A1 (en) 2016-05-12

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