KR20170078654A - 코판리십 및 그의 디히드로클로라이드 염의 합성 - Google Patents

코판리십 및 그의 디히드로클로라이드 염의 합성 Download PDF

Info

Publication number
KR20170078654A
KR20170078654A KR1020177011704A KR20177011704A KR20170078654A KR 20170078654 A KR20170078654 A KR 20170078654A KR 1020177011704 A KR1020177011704 A KR 1020177011704A KR 20177011704 A KR20177011704 A KR 20177011704A KR 20170078654 A KR20170078654 A KR 20170078654A
Authority
KR
South Korea
Prior art keywords
formula
compound
optionally
rti
solvent
Prior art date
Application number
KR1020177011704A
Other languages
English (en)
Korean (ko)
Other versions
KR102562286B1 (ko
Inventor
얀-게오르크 페테르스
위르겐 슈티엘
카이 로비스
Original Assignee
바이엘 파마 악티엔게젤샤프트
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 바이엘 파마 악티엔게젤샤프트 filed Critical 바이엘 파마 악티엔게젤샤프트
Publication of KR20170078654A publication Critical patent/KR20170078654A/ko
Application granted granted Critical
Publication of KR102562286B1 publication Critical patent/KR102562286B1/ko

Links

Classifications

    • 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
    • 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
    • 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
KR1020177011704A 2014-11-07 2015-11-05 코판리십 및 그의 디히드로클로라이드 염의 합성 KR102562286B1 (ko)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
KR20170078654A true KR20170078654A (ko) 2017-07-07
KR102562286B1 KR102562286B1 (ko) 2023-08-02

Family

ID=51866060

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177011704A KR102562286B1 (ko) 2014-11-07 2015-11-05 코판리십 및 그의 디히드로클로라이드 염의 합성

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
ES2708350T3 (es) 2013-04-08 2019-04-09 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas para el tratamiento de linfomas
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
CN108884098B (zh) 2016-03-08 2021-09-14 拜耳制药股份公司 2-氨基-N-[7-甲氧基-2,3-二氢咪唑并[1,2-c]喹唑啉-5-基]嘧啶-5-甲酰胺类
CN109729716B (zh) 2016-09-23 2022-03-15 拜耳制药股份公司 Pi3k-抑制剂的组合产品
US11185549B2 (en) 2017-06-28 2021-11-30 Bayer Consumer Care Ag Combination of a PI3K-inhibitor with an androgen receptor antagonist

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008070150A1 (en) * 2006-12-05 2008-06-12 Bayer Schering Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
WO2012136553A1 (en) * 2011-04-05 2012-10-11 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts

Family Cites Families (6)

* 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
US7375232B2 (en) * 2001-08-15 2008-05-20 E.I. Du Pont De Nemours And Company Ortho-heterocyclic substituted aryl amides for controlling invertebrate pests
KR101059652B1 (ko) 2002-09-30 2011-08-25 바이엘 파마 악티엔게젤샤프트 접합 아졸-피리미딘 유도체
WO2009091550A2 (en) * 2008-01-14 2009-07-23 Bayer Healthcare Llc Sulfone substituted 2,3-dihydroimidazo [1,2-c] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis
MY156209A (en) 2009-11-04 2016-01-29 Novartis Ag Heterocyclic sulfonamide derivatives useful mek inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008070150A1 (en) * 2006-12-05 2008-06-12 Bayer Schering Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
WO2012136553A1 (en) * 2011-04-05 2012-10-11 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts

Also Published As

Publication number Publication date
CA2966796A1 (en) 2016-05-12
ZA201703866B (en) 2019-06-26
EP3215507B1 (en) 2018-12-26
CN107074776A (zh) 2017-08-18
RS58494B1 (sr) 2019-04-30
MX365111B (es) 2019-05-23
WO2016071426A1 (en) 2016-05-12
EA201790982A1 (ru) 2017-10-31
BR112017009471B1 (pt) 2023-02-28
TW201625633A (zh) 2016-07-16
EP3018131A1 (en) 2016-05-11
AU2015341779A1 (en) 2017-05-11
ES2716730T3 (es) 2019-06-14
MY183123A (en) 2021-02-15
SI3215507T1 (sl) 2019-04-30
JO3487B1 (ar) 2020-07-05
CO2017004533A2 (es) 2017-07-19
NZ730843A (en) 2022-12-23
IL251586A0 (en) 2017-06-29
MX2017005891A (es) 2017-06-30
CA2966796C (en) 2022-12-06
UY36396A (es) 2016-06-30
UA118999C2 (uk) 2019-04-10
TWI697494B (zh) 2020-07-01
CN107074776B (zh) 2021-02-02
PT3215507T (pt) 2019-03-29
IL251586B (en) 2019-05-30
AR102568A1 (es) 2017-03-08
KR102562286B1 (ko) 2023-08-02
US10035803B2 (en) 2018-07-31
EA031248B1 (ru) 2018-12-28
BR112017009471A2 (pt) 2018-01-02
JP6691114B2 (ja) 2020-04-28
PE20170951A1 (es) 2017-07-13
AU2015341779B2 (en) 2020-02-27
DK3215507T3 (en) 2019-04-15
HRP20190527T1 (hr) 2019-05-17
JP2017536352A (ja) 2017-12-07
HRP20190527T8 (hr) 2020-02-21
HUE042794T2 (hu) 2019-07-29
LT3215507T (lt) 2019-04-10
US20170327505A1 (en) 2017-11-16
EP3215507A1 (en) 2017-09-13
PL3215507T3 (pl) 2019-08-30
CL2017001130A1 (es) 2018-01-19
TR201904346T4 (tr) 2019-04-22
SG11201702999XA (en) 2017-05-30

Similar Documents

Publication Publication Date Title
KR102562286B1 (ko) 코판리십 및 그의 디히드로클로라이드 염의 합성
EP3215493B1 (en) Synthesis of copanlisib and its dihydrochloride salt
KR20180137496A (ko) 인다졸의 합성
TWI716060B (zh) 用於合成2-羥基喹㗁啉的區域選擇性一步驟方法
WO2016071382A1 (en) Synthesis of pi3k inhibitor and salts thereof
CN111606910A (zh) 一种抗肿瘤药物Sapanisertib的合成工艺
CN113444023B (zh) 一种叔丁氧羰基保护的氨类化合物的合成方法及应用
Zhou et al. Synthesis and analysis of 1-methyl-4-phenyl-1H-imidazol-2-amine
WO2016071380A1 (en) Synthesis of pi3k inhibitor and salts thereof

Legal Events

Date Code Title Description
A201 Request for examination
E902 Notification of reason for refusal
E701 Decision to grant or registration of patent right