SG11201702999XA - Synthesis of copanlisib and its dihydrochloride salt - Google Patents

Synthesis of copanlisib and its dihydrochloride salt

Info

Publication number
SG11201702999XA
SG11201702999XA SG11201702999XA SG11201702999XA SG11201702999XA SG 11201702999X A SG11201702999X A SG 11201702999XA SG 11201702999X A SG11201702999X A SG 11201702999XA SG 11201702999X A SG11201702999X A SG 11201702999XA SG 11201702999X A SG11201702999X A SG 11201702999XA
Authority
SG
Singapore
Prior art keywords
copanlisib
synthesis
dihydrochloride salt
dihydrochloride
salt
Prior art date
Application number
SG11201702999XA
Other languages
English (en)
Inventor
Jan-Georg Peters
Jürgen Stiehl
Kai Lovis
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 SG11201702999XA publication Critical patent/SG11201702999XA/en

Links

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
    • C07D233/24Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
SG11201702999XA 2014-11-07 2015-11-05 Synthesis of copanlisib and its dihydrochloride salt SG11201702999XA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14192202.1A EP3018131A1 (en) 2014-11-07 2014-11-07 Synthesis of copanlisib and its dihydrochloride salt
PCT/EP2015/075765 WO2016071426A1 (en) 2014-11-07 2015-11-05 Synthesis of copanlisib and its dihydrochloride salt

Publications (1)

Publication Number Publication Date
SG11201702999XA true SG11201702999XA (en) 2017-05-30

Family

ID=51866060

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201702999XA SG11201702999XA (en) 2014-11-07 2015-11-05 Synthesis of copanlisib and its dihydrochloride salt

Country Status (34)

Country Link
US (1) US10035803B2 (und)
EP (2) EP3018131A1 (und)
JP (1) JP6691114B2 (und)
KR (1) KR102562286B1 (und)
CN (1) CN107074776B (und)
AR (1) AR102568A1 (und)
AU (1) AU2015341779B2 (und)
BR (1) BR112017009471B1 (und)
CA (1) CA2966796C (und)
CL (1) CL2017001130A1 (und)
CO (1) CO2017004533A2 (und)
DK (1) DK3215507T3 (und)
EA (1) EA031248B1 (und)
ES (1) ES2716730T3 (und)
HR (1) HRP20190527T8 (und)
HU (1) HUE042794T2 (und)
IL (1) IL251586B (und)
JO (1) JO3487B1 (und)
LT (1) LT3215507T (und)
MX (1) MX365111B (und)
MY (1) MY183123A (und)
NZ (1) NZ730843A (und)
PE (1) PE20170951A1 (und)
PL (1) PL3215507T3 (und)
PT (1) PT3215507T (und)
RS (1) RS58494B1 (und)
SG (1) SG11201702999XA (und)
SI (1) SI3215507T1 (und)
TR (1) TR201904346T4 (und)
TW (1) TWI697494B (und)
UA (1) UA118999C2 (und)
UY (1) UY36396A (und)
WO (1) WO2016071426A1 (und)
ZA (1) ZA201703866B (und)

Families Citing this family (9)

* 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
WO2014166820A1 (en) 2013-04-08 2014-10-16 Bayer Pharma Aktiengesllschaft Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas
EP3018127A1 (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
CN105130998B (zh) * 2015-09-25 2017-07-28 苏州立新制药有限公司 库潘尼西的制备方法
WO2017153220A1 (en) 2016-03-08 2017-09-14 Bayer Pharma Aktiengesellschaft 2—amino—n— [7—methoxy—2, 3-dihydroimidazo-[1, 2-c] quinazolin-5-yl] pyrimidine—5—carboxamides
WO2018054782A1 (en) 2016-09-23 2018-03-29 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors
EP3645005A1 (en) 2017-06-28 2020-05-06 Bayer Consumer Care AG Combination of a pi3k-inhibitor with an androgen receptor antagonist

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN100506817C (zh) * 2001-08-15 2009-07-01 纳幕尔杜邦公司 用于防治无脊椎害虫的邻-杂环取代的芳基酰胺类化合物
MXPA05001808A (es) 2002-09-30 2005-08-16 Bayer Pharmaceuticals Corp Derivados de azol-pirimidina condensados.
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
EP2244721A4 (en) * 2008-01-14 2017-01-18 Bayer Intellectual Property GmbH Sulfone substituted 2,3-dihydroimidazo ý1,2-c¨quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis
AU2010317167B2 (en) 2009-11-04 2012-11-29 Novartis Ag Heterocyclic sulfonamide derivatives useful as MEK inhibitors
EP2508525A1 (en) * 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts

Also Published As

Publication number Publication date
CA2966796C (en) 2022-12-06
US20170327505A1 (en) 2017-11-16
LT3215507T (lt) 2019-04-10
PE20170951A1 (es) 2017-07-13
CN107074776B (zh) 2021-02-02
JP2017536352A (ja) 2017-12-07
AU2015341779B2 (en) 2020-02-27
DK3215507T3 (en) 2019-04-15
EP3215507B1 (en) 2018-12-26
PT3215507T (pt) 2019-03-29
ES2716730T3 (es) 2019-06-14
KR20170078654A (ko) 2017-07-07
EA031248B1 (ru) 2018-12-28
HUE042794T2 (hu) 2019-07-29
TW201625633A (zh) 2016-07-16
RS58494B1 (sr) 2019-04-30
EA201790982A1 (ru) 2017-10-31
HRP20190527T8 (hr) 2020-02-21
BR112017009471A2 (pt) 2018-01-02
TR201904346T4 (tr) 2019-04-22
WO2016071426A1 (en) 2016-05-12
MX365111B (es) 2019-05-23
PL3215507T3 (pl) 2019-08-30
MY183123A (en) 2021-02-15
SI3215507T1 (sl) 2019-04-30
CL2017001130A1 (es) 2018-01-19
JP6691114B2 (ja) 2020-04-28
EP3018131A1 (en) 2016-05-11
IL251586B (en) 2019-05-30
IL251586A0 (en) 2017-06-29
JO3487B1 (ar) 2020-07-05
MX2017005891A (es) 2017-06-30
CA2966796A1 (en) 2016-05-12
ZA201703866B (en) 2019-06-26
HRP20190527T1 (hr) 2019-05-17
AR102568A1 (es) 2017-03-08
KR102562286B1 (ko) 2023-08-02
UA118999C2 (uk) 2019-04-10
EP3215507A1 (en) 2017-09-13
US10035803B2 (en) 2018-07-31
BR112017009471B1 (pt) 2023-02-28
CO2017004533A2 (es) 2017-07-19
TWI697494B (zh) 2020-07-01
CN107074776A (zh) 2017-08-18
UY36396A (es) 2016-06-30
NZ730843A (en) 2022-12-23
AU2015341779A1 (en) 2017-05-11

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