CN103649091A - 取代的2,3-二氢咪唑并[1,2-c]喹唑啉盐 - Google Patents

取代的2,3-二氢咪唑并[1,2-c]喹唑啉盐 Download PDF

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Publication number
CN103649091A
CN103649091A CN201280027509.4A CN201280027509A CN103649091A CN 103649091 A CN103649091 A CN 103649091A CN 201280027509 A CN201280027509 A CN 201280027509A CN 103649091 A CN103649091 A CN 103649091A
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dihydrochloride
cancer
mixture
formula
optionally
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Chinese (zh)
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CN103649091B (zh
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J·G·彼得斯
H-C·米利策尔
H·米勒
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Bayer Pharma AG
Bayer Intellectual Property GmbH
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Bayer Pharma AG
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
CN201280027509.4A 2011-04-05 2012-03-29 取代的2,3-二氢咪唑并[1,2-c]喹唑啉盐 Active CN103649091B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11161111.7 2011-04-05
EP11161111A EP2508525A1 (en) 2011-04-05 2011-04-05 Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts
PCT/EP2012/055600 WO2012136553A1 (en) 2011-04-05 2012-03-29 Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts

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CN103649091A true CN103649091A (zh) 2014-03-19
CN103649091B CN103649091B (zh) 2016-06-22

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US (2) US10383876B2 (und)
EP (2) EP2508525A1 (und)
JP (2) JP5763834B2 (und)
KR (1) KR101937501B1 (und)
CN (1) CN103649091B (und)
AP (1) AP3709A (und)
AR (1) AR085718A1 (und)
AU (1) AU2012238891B2 (und)
BR (1) BR112013025549A2 (und)
CA (1) CA2832123C (und)
CL (1) CL2013002870A1 (und)
CO (1) CO6781534A2 (und)
CR (1) CR20130511A (und)
CU (1) CU24208B1 (und)
CY (1) CY1116231T1 (und)
DK (1) DK2694508T3 (und)
DO (1) DOP2013000223A (und)
EA (1) EA023646B1 (und)
EC (1) ECSP13013006A (und)
ES (1) ES2529653T3 (und)
GT (1) GT201300234A (und)
HK (1) HK1195907A1 (und)
HR (1) HRP20150138T1 (und)
IL (1) IL228561A (und)
JO (1) JO2958B1 (und)
MA (1) MA35014B1 (und)
ME (1) ME02021B (und)
MX (1) MX336057B (und)
MY (1) MY169452A (und)
PE (1) PE20141038A1 (und)
PL (1) PL2694508T3 (und)
PT (1) PT2694508E (und)
RS (1) RS53811B1 (und)
SG (1) SG193595A1 (und)
SI (1) SI2694508T1 (und)
SM (1) SMT201500037B (und)
TN (1) TN2013000401A1 (und)
TW (2) TWI549954B (und)
UA (1) UA111604C2 (und)
UY (1) UY33985A (und)
WO (1) WO2012136553A1 (und)
ZA (1) ZA201307105B (und)

Cited By (4)

* Cited by examiner, † Cited by third party
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CN107074776A (zh) * 2014-11-07 2017-08-18 拜耳制药股份公司 Copanlisib及其二盐酸盐的合成
CN107864625A (zh) * 2015-03-09 2018-03-30 拜耳制药股份公司 含有取代的2,3‑二氢咪唑并[1,2‑c]喹唑啉的组合产品
CN112930212A (zh) * 2018-10-17 2021-06-08 桑多斯股份公司 包含左甲状腺素和二羧酸的共晶体
CN113260365A (zh) * 2018-12-27 2021-08-13 治愈医药社株式会社 新型化合物及包含其的用于增强抗癌活性的药学组合物

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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
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
CU24400B1 (es) * 2013-04-08 2019-04-04 Bayer Pharma AG Una composición que comprende 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas
CA2915311A1 (en) 2013-06-14 2014-12-18 Bayer Pharma Aktiengesellschaft Anti-tweakr antibodies and uses thereof
CN103694319B (zh) * 2013-12-20 2018-02-27 深圳翰宇药业股份有限公司 一种布舍瑞林的纯化方法
EP3018127A1 (en) * 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
MX2017011607A (es) * 2015-03-09 2018-04-10 Bayer Pharma AG Uso de 2,3-dihidroimidazol[1,2-c]quinazolinas sustituidas.
HUE048111T2 (hu) 2015-03-23 2020-05-28 Bayer Pharma AG Anti-CEACAM6 ellenanyagok és alkalmazásuk
EP3280448B1 (en) 2015-04-10 2020-12-30 Capsugel Belgium NV Abiraterone acetate lipid formulations
WO2017134000A1 (en) 2016-02-01 2017-08-10 Bayer Pharma Aktiengesellschaft Copanlisib biomarkers
KR20180104129A (ko) 2016-02-01 2018-09-19 바이엘 파마 악티엔게젤샤프트 코판리십 바이오마커
MY189113A (en) 2016-03-02 2022-01-26 Eisai R&D Man Co Ltd Eribulin-based antibody-drug conjugates and methods of use
CA3016584A1 (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
EP3219329A1 (en) 2016-03-17 2017-09-20 Bayer Pharma Aktiengesellschaft Combinations of copanlisib
CA3037626A1 (en) 2016-09-23 2018-03-29 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors
JP2020503289A (ja) 2016-12-14 2020-01-30 ターベダ セラピューティクス インコーポレイテッドTarveda Therapeutics,Inc. Hsp90標的化コンジュゲート及びその製剤
EP3585437B1 (en) 2017-02-24 2022-12-21 Bayer Pharma Aktiengesellschaft Combinations of copanlisib with anti-pd-1 antibody
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
DK3678644T3 (da) * 2017-09-08 2023-07-31 Bayer Pharma AG Formuleringer af copanlisib
WO2019105734A1 (en) 2017-11-28 2019-06-06 Bayer Consumer Care Ag Combinations of copanlisib
WO2019105835A1 (en) 2017-11-29 2019-06-06 Bayer Consumer Care Ag Combinations of copanlisib and anetumab ravtansine
WO2019197269A1 (en) 2018-04-11 2019-10-17 Bayer Aktiengesellschaft Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer
WO2020043617A1 (en) 2018-08-28 2020-03-05 Bayer As Combination of pi3k-inhibitors and targeted thorium conjugates
US20210369724A1 (en) * 2018-10-16 2021-12-02 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
WO2020164997A1 (en) 2019-02-12 2020-08-20 Bayer Aktiengesellschaft Combination of pi3k-inhibitors
WO2023218032A1 (en) 2022-05-13 2023-11-16 Synthon B.V. Solid forms of copanlisib salts

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WO2010034414A1 (en) * 2008-09-24 2010-04-01 Bayer Schering Pharma Aktiengesellschaft Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma

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JO3733B1 (ar) * 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
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MX2017011607A (es) * 2015-03-09 2018-04-10 Bayer Pharma AG Uso de 2,3-dihidroimidazol[1,2-c]quinazolinas sustituidas.
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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
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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107074776A (zh) * 2014-11-07 2017-08-18 拜耳制药股份公司 Copanlisib及其二盐酸盐的合成
CN107074776B (zh) * 2014-11-07 2021-02-02 拜耳制药股份公司 Copanlisib及其二盐酸盐的合成
CN107864625A (zh) * 2015-03-09 2018-03-30 拜耳制药股份公司 含有取代的2,3‑二氢咪唑并[1,2‑c]喹唑啉的组合产品
CN112930212A (zh) * 2018-10-17 2021-06-08 桑多斯股份公司 包含左甲状腺素和二羧酸的共晶体
CN113260365A (zh) * 2018-12-27 2021-08-13 治愈医药社株式会社 新型化合物及包含其的用于增强抗癌活性的药学组合物

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UY33985A (es) 2012-10-31
SG193595A1 (en) 2013-10-30
PE20141038A1 (es) 2014-09-05
US20140072529A1 (en) 2014-03-13
ZA201307105B (en) 2014-11-26
SMT201500037B (it) 2015-05-05
US10383876B2 (en) 2019-08-20
KR20140021637A (ko) 2014-02-20
TWI592158B (zh) 2017-07-21
JP5826961B2 (ja) 2015-12-02
AR085718A1 (es) 2013-10-23
CR20130511A (es) 2013-12-04
PL2694508T3 (pl) 2015-04-30
JO2958B1 (en) 2016-03-15
UA111604C2 (uk) 2016-05-25
PT2694508E (pt) 2015-02-10
JP2014510119A (ja) 2014-04-24
JP2015164936A (ja) 2015-09-17
EA201391470A1 (ru) 2014-03-31
WO2012136553A1 (en) 2012-10-11
EP2694508A1 (en) 2014-02-12
CU24208B1 (es) 2016-11-29
EP2508525A1 (en) 2012-10-10
ECSP13013006A (es) 2013-12-31
CA2832123C (en) 2018-09-11
CN103649091B (zh) 2016-06-22
GT201300234A (es) 2015-01-16
CO6781534A2 (es) 2013-10-31
MA35014B1 (fr) 2014-04-03
US9636344B2 (en) 2017-05-02
NZ616198A (en) 2015-09-25
EA023646B1 (ru) 2016-06-30
IL228561A0 (en) 2013-12-31
AU2012238891A1 (en) 2013-10-24
AU2012238891B2 (en) 2016-12-01
MY169452A (en) 2019-04-11
HRP20150138T1 (hr) 2015-05-08
JP5763834B2 (ja) 2015-08-12
CU20130133A7 (es) 2014-01-29
CL2013002870A1 (es) 2014-06-20
DOP2013000223A (es) 2013-11-15
HK1195907A1 (zh) 2014-11-28
TWI549954B (zh) 2016-09-21
MX2013011583A (es) 2013-12-16
EP2694508B1 (en) 2014-11-19
US20160193219A1 (en) 2016-07-07
TN2013000401A1 (en) 2015-03-30
AP2013007219A0 (en) 2013-10-31
DK2694508T3 (en) 2015-02-16
TW201249847A (en) 2012-12-16
CY1116231T1 (el) 2017-02-08
BR112013025549A2 (pt) 2016-12-27
MX336057B (es) 2016-01-07
KR101937501B1 (ko) 2019-01-10
RS53811B1 (en) 2015-06-30
AP3709A (en) 2016-05-31
ME02021B (me) 2015-05-20
TW201637656A (zh) 2016-11-01
CA2832123A1 (en) 2012-10-11
ES2529653T3 (es) 2015-02-24
SI2694508T1 (sl) 2015-03-31
IL228561A (en) 2015-10-29

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