CA2832123C - Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts - Google Patents

Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts Download PDF

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Publication number
CA2832123C
CA2832123C CA2832123A CA2832123A CA2832123C CA 2832123 C CA2832123 C CA 2832123C CA 2832123 A CA2832123 A CA 2832123A CA 2832123 A CA2832123 A CA 2832123A CA 2832123 C CA2832123 C CA 2832123C
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Prior art keywords
formula
dihydrochloride salt
mixture
cancer
salt
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CA2832123A
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English (en)
French (fr)
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CA2832123A1 (en
Inventor
Jan Georg Peters
Hans-Christian Militzer
Hartwig Muller
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Bayer Intellectual Property GmbH
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Bayer Intellectual Property GmbH
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Publication of CA2832123A1 publication Critical patent/CA2832123A1/en
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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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2832123A 2011-04-05 2012-03-29 Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts Active CA2832123C (en)

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

Publications (2)

Publication Number Publication Date
CA2832123A1 CA2832123A1 (en) 2012-10-11
CA2832123C true CA2832123C (en) 2018-09-11

Family

ID=43984137

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2832123A Active CA2832123C (en) 2011-04-05 2012-03-29 Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts

Country Status (42)

Country Link
US (2) US10383876B2 (https=)
EP (2) EP2508525A1 (https=)
JP (2) JP5763834B2 (https=)
KR (1) KR101937501B1 (https=)
CN (1) CN103649091B (https=)
AP (1) AP3709A (https=)
AR (1) AR085718A1 (https=)
AU (1) AU2012238891B2 (https=)
BR (1) BR112013025549A2 (https=)
CA (1) CA2832123C (https=)
CL (1) CL2013002870A1 (https=)
CO (1) CO6781534A2 (https=)
CR (1) CR20130511A (https=)
CU (1) CU24208B1 (https=)
CY (1) CY1116231T1 (https=)
DK (1) DK2694508T3 (https=)
DO (1) DOP2013000223A (https=)
EA (1) EA023646B1 (https=)
EC (1) ECSP13013006A (https=)
ES (1) ES2529653T3 (https=)
GT (1) GT201300234A (https=)
HR (1) HRP20150138T1 (https=)
IL (1) IL228561A (https=)
JO (1) JO2958B1 (https=)
MA (1) MA35014B1 (https=)
ME (1) ME02021B (https=)
MX (1) MX336057B (https=)
MY (1) MY169452A (https=)
PE (1) PE20141038A1 (https=)
PH (1) PH12013502065A1 (https=)
PL (1) PL2694508T3 (https=)
PT (1) PT2694508E (https=)
RS (1) RS53811B1 (https=)
SG (1) SG193595A1 (https=)
SI (1) SI2694508T1 (https=)
SM (1) SMT201500037B (https=)
TN (1) TN2013000401A1 (https=)
TW (2) TWI549954B (https=)
UA (1) UA111604C2 (https=)
UY (1) UY33985A (https=)
WO (1) WO2012136553A1 (https=)
ZA (1) ZA201307105B (https=)

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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
MX2015014171A (es) * 2013-04-08 2015-12-16 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas.
SG11201509116VA (en) 2013-06-14 2015-12-30 Bayer Pharma AG 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
EP3018131A1 (en) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
AU2016231260A1 (en) * 2015-03-09 2017-09-21 Bayer Healthcare Pharmaceuticals Inc. Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines
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
PT3274370T (pt) 2015-03-23 2020-01-30 Bayer Pharma AG Anticorpos anti-ceacam6 e utilizações dos mesmos
ES2863500T3 (es) 2015-04-10 2021-10-11 Capsugel Belgium Nv Formulaciones lipídicas de acetato de abiraterona
MX2018009368A (es) 2016-02-01 2018-09-05 Bayer Pharma AG Biomarcadores para copanlisib.
AU2017215096A1 (en) 2016-02-01 2018-08-09 Bayer Pharma Aktiengesellschaft Copanlisib biomarkers
EP3423105B1 (en) 2016-03-02 2021-05-05 Eisai R&D Management 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
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
US11241500B2 (en) 2016-12-14 2022-02-08 Tarveda Therapeutics, Inc. HSP90-targeting conjugates and formulations thereof
US11684672B2 (en) 2017-02-24 2023-06-27 Bayer Pharma Aktiengesellschaft Combinations of copanlisib with anti-PD-1 antibody
EP3645005A1 (en) 2017-06-28 2020-05-06 Bayer Consumer Care AG Combination of a pi3k-inhibitor with an androgen receptor antagonist
EP3498266A1 (en) 2017-12-15 2019-06-19 Bayer Consumer Care AG Formulations of copanlisib
JP2020533292A (ja) 2017-09-08 2020-11-19 バイエル・コンシューマー・ケア・アクチェンゲゼルシャフトBayer Consumer Care AG コパンリシブの製剤
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
EP3843743A1 (en) 2018-08-28 2021-07-07 Bayer AS Combination of pi3k-inhibitors and targeted thorium conjugates
EP3866805A1 (en) * 2018-10-16 2021-08-25 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
EP3866923A1 (en) * 2018-10-17 2021-08-25 Sandoz AG Co-crystals comprising levothyroxine and a dicarboxylic acid
AU2019416623B2 (en) * 2018-12-27 2022-12-08 Holosmedic Novel compound and pharmaceutical composition comprising same for enhancing anticancer activity
WO2020164997A1 (en) 2019-02-12 2020-08-20 Bayer Aktiengesellschaft Combination of pi3k-inhibitors
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WO2025053315A1 (ko) * 2023-09-08 2025-03-13 파로스젠 주식회사 항암제 프로드러그 컨쥬게이트의 제조에서 팔라듐의 회수 및 제거 방법

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JO3733B1 (ar) * 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
MX2015014171A (es) 2013-04-08 2015-12-16 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas.
WO2015082322A1 (en) 2013-12-03 2015-06-11 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
EP3018127A1 (en) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
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
AU2016231260A1 (en) * 2015-03-09 2017-09-21 Bayer Healthcare Pharmaceuticals Inc. Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines

Also Published As

Publication number Publication date
TWI549954B (zh) 2016-09-21
IL228561A0 (en) 2013-12-31
TWI592158B (zh) 2017-07-21
SG193595A1 (en) 2013-10-30
EP2508525A1 (en) 2012-10-10
PE20141038A1 (es) 2014-09-05
KR101937501B1 (ko) 2019-01-10
AU2012238891A1 (en) 2013-10-24
ME02021B (me) 2015-05-20
WO2012136553A1 (en) 2012-10-11
JP5826961B2 (ja) 2015-12-02
EP2694508B1 (en) 2014-11-19
IL228561A (en) 2015-10-29
EA023646B1 (ru) 2016-06-30
PT2694508E (pt) 2015-02-10
UA111604C2 (uk) 2016-05-25
PL2694508T3 (pl) 2015-04-30
CN103649091B (zh) 2016-06-22
CL2013002870A1 (es) 2014-06-20
AU2012238891B2 (en) 2016-12-01
US9636344B2 (en) 2017-05-02
SI2694508T1 (sl) 2015-03-31
HRP20150138T1 (hr) 2015-05-08
CR20130511A (es) 2013-12-04
TN2013000401A1 (en) 2015-03-30
ZA201307105B (en) 2014-11-26
CA2832123A1 (en) 2012-10-11
EA201391470A1 (ru) 2014-03-31
CY1116231T1 (el) 2017-02-08
MY169452A (en) 2019-04-11
BR112013025549A2 (pt) 2016-12-27
CO6781534A2 (es) 2013-10-31
AR085718A1 (es) 2013-10-23
CU24208B1 (es) 2016-11-29
EP2694508A1 (en) 2014-02-12
PH12013502065A1 (en) 2016-06-29
GT201300234A (es) 2015-01-16
JP5763834B2 (ja) 2015-08-12
AP2013007219A0 (en) 2013-10-31
AP3709A (en) 2016-05-31
MA35014B1 (fr) 2014-04-03
TW201249847A (en) 2012-12-16
ECSP13013006A (es) 2013-12-31
TW201637656A (zh) 2016-11-01
CN103649091A (zh) 2014-03-19
NZ616198A (en) 2015-09-25
MX336057B (es) 2016-01-07
RS53811B1 (sr) 2015-06-30
MX2013011583A (es) 2013-12-16
JP2015164936A (ja) 2015-09-17
HK1195907A1 (zh) 2014-11-28
KR20140021637A (ko) 2014-02-20
DOP2013000223A (es) 2013-11-15
US20140072529A1 (en) 2014-03-13
SMT201500037B (it) 2015-05-05
US10383876B2 (en) 2019-08-20
US20160193219A1 (en) 2016-07-07
JO2958B1 (en) 2016-03-15
CU20130133A7 (es) 2014-01-29
UY33985A (es) 2012-10-31
JP2014510119A (ja) 2014-04-24
ES2529653T3 (es) 2015-02-24
DK2694508T3 (en) 2015-02-16

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