JO3644B1 - تخليق كوبانليسيب وملح الدايهيدروكلوريد الخاص به - Google Patents

تخليق كوبانليسيب وملح الدايهيدروكلوريد الخاص به

Info

Publication number
JO3644B1
JO3644B1 JOP/2015/0274A JOP20150274A JO3644B1 JO 3644 B1 JO3644 B1 JO 3644B1 JO P20150274 A JOP20150274 A JO P20150274A JO 3644 B1 JO3644 B1 JO 3644B1
Authority
JO
Jordan
Prior art keywords
copanlisib
synthesis
dihydrochloride salt
dihydrochloride
hydrates
Prior art date
Application number
JOP/2015/0274A
Other languages
English (en)
Inventor
Andreas Lender Dr
Kai Lovis Dr
Franz-Josef Mais Dr
Philipp Rubenbauer Dr
Goetz Daniel
Danja Gro?Bach Dr
Heiko Schirmer Dr
Seyfried Martin
Marty Maurus
Jan-Georg Peters Dr
Stiehl Juergen
Zweifel Theodor
Weing?Rtner G?Nter
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
Application granted granted Critical
Publication of JO3644B1 publication Critical patent/JO3644B1/ar

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/08—Heterocyclic 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
    • C07D295/084—Heterocyclic 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
    • C07D295/088—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

يتعلق الاختراع الحالي بطريقة جديدة لتحضير copanlisib، copanlisibdihydrochloride، أو hydrates من copanlisibdihydrochloride، بمركبات وسطية جديدة، وباستخدام المركبات الوسطية الجديدة المذكورة لتحضير copanlisib، copanlisibdihydrochloride، أو hydrates من copanlisibdihydrochloride المذكورين. يتعلق الاختراع الحالي أيضا مع copanlisibdihydrochloride hydrates كمركبات.
JOP/2015/0274A 2014-11-07 2015-11-04 تخليق كوبانليسيب وملح الدايهيدروكلوريد الخاص به JO3644B1 (ar)

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
JO3644B1 true JO3644B1 (ar) 2020-08-27

Family

ID=51866061

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2015/0274A JO3644B1 (ar) 2014-11-07 2015-11-04 تخليق كوبانليسيب وملح الدايهيدروكلوريد الخاص به

Country Status (46)

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

Families Citing this family (12)

* 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
UA119537C2 (uk) 2013-04-08 2019-07-10 Байєр Фарма Акцієнгезелльшафт ЗАСТОСУВАННЯ ЗАМІЩЕНИХ 2,3-ДИГІДРОІМІДАЗО[1,2-c]ХІНАЗОЛІНІВ ДЛЯ ЛІКУВАННЯ ЛІМФОМ
CA2978830A1 (en) 2015-03-09 2016-09-15 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations
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
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
EP3498266A1 (en) 2017-12-15 2019-06-19 Bayer Consumer Care AG Formulations of copanlisib
CN111278430A (zh) 2017-09-08 2020-06-12 拜耳制药股份公司 库潘尼西制剂
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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US6221877B1 (en) * 2000-04-12 2001-04-24 Regents Of The University Of California Substituted 4-phthalimidocarboxanilides as inhibitors of purine salvage phosphoribosyltransferases
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
EP1417204B1 (en) * 2001-08-15 2006-01-18 E. I. du Pont de Nemours and Company Ortho-heterocyclic substituted aryl amides for controlling invertebrate pests
AU2003293310B2 (en) 2002-09-30 2010-04-01 Bayer Intellectual Property Gmbh Fused azole-pyrimidine derivatives
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
JP5620275B2 (ja) * 2008-01-14 2014-11-05 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 超増殖性疾患及び脈管形成に関連する疾病を処理するために有用なスルホン置換された２，３−ジヒドロイミダゾ［１，２−ｃ］キナゾリン誘導体類
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
UA119537C2 (uk) 2013-04-08 2019-07-10 Байєр Фарма Акцієнгезелльшафт ЗАСТОСУВАННЯ ЗАМІЩЕНИХ 2,3-ДИГІДРОІМІДАЗО[1,2-c]ХІНАЗОЛІНІВ ДЛЯ ЛІКУВАННЯ ЛІМФОМ
JP6499657B2 (ja) 2013-12-03 2019-04-10 バイエル ファーマ アクチエンゲゼルシャフト Ｐｉ３ｋ阻害剤の組み合わせ
EP3018131A1 (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
JP2018512403A (ja) 2015-03-09 2018-05-17 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］キナゾリン類の使用
CA3012951A1 (en) 2016-02-01 2017-08-10 Bayer Pharma Aktiengesellschaft Copanlisib biomarkers
EP3411497A1 (en) 2016-02-01 2018-12-12 Bayer Pharma Aktiengesellschaft Copanlisib biomarkers
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
CA3037626A1 (en) 2016-09-23 2018-03-29 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors

Also Published As

Publication number Publication date
MA40895A (fr) 2017-09-13
MA40895B1 (fr) 2019-07-31
EA035558B1 (ru) 2020-07-07
EP3215493B1 (en) 2019-01-23
HUE042866T2 (hu) 2019-07-29
AR102570A1 (es) 2017-03-08
HRP20190720T1 (hr) 2019-06-14
PE20170897A1 (es) 2017-07-12
NI201700054A (es) 2017-07-17
PH12017500833A1 (en) 2017-10-18
TR201905217T4 (tr) 2019-05-21
HK1245774A1 (zh) 2018-08-31
NZ731287A (en) 2023-01-27
CA2966800A1 (en) 2016-05-12
DK3215493T3 (da) 2019-05-06
WO2016071435A3 (en) 2016-06-30
CY1121602T1 (el) 2020-05-29
UA122398C2 (uk) 2020-11-10
ME03358B (me) 2019-10-20
CN107278204B (zh) 2019-12-17
KR20170082563A (ko) 2017-07-14
SA517381462B1 (ar) 2021-01-25
CO2017004532A2 (es) 2017-07-19
TN2017000179A1 (en) 2018-10-19
CU20170061A7 (es) 2017-10-05
PT3215493T (pt) 2019-05-21
AU2015341788A1 (en) 2017-05-18
AU2015341788B2 (en) 2020-01-16
US20180282337A1 (en) 2018-10-04
MX366904B (es) 2019-07-30
BR112017009470B1 (pt) 2022-11-01
CU24489B1 (es) 2020-12-17
CN107278204A (zh) 2017-10-20
CL2017001131A1 (es) 2018-01-19
EP3018127A1 (en) 2016-05-11
BR112017009470A2 (en) 2018-01-02
SG11201703702RA (en) 2017-06-29
MY189852A (en) 2022-03-14
ZA201703867B (en) 2019-07-31
EP3215493A2 (en) 2017-09-13
CR20170184A (es) 2017-06-20
US10494372B2 (en) 2019-12-03
IL251874A0 (en) 2017-06-29
ECSP17027755A (es) 2017-06-30
SV2017005433A (es) 2018-04-30
MX2017005893A (es) 2017-06-30
KR102566834B1 (ko) 2023-08-16
JP6691115B2 (ja) 2020-04-28
ES2721778T3 (es) 2019-08-05
SI3215493T1 (sl) 2019-05-31
DOP2017000112A (es) 2017-06-15
CA2966800C (en) 2023-02-21
PL3215493T3 (pl) 2019-07-31
UY36392A (es) 2016-06-30
TWI697495B (zh) 2020-07-01
LT3215493T (lt) 2019-04-25
JP2017534631A (ja) 2017-11-24
RS58579B1 (sr) 2019-05-31
WO2016071435A2 (en) 2016-05-12
TW201625634A (zh) 2016-07-16
EA201790983A1 (ru) 2017-10-31

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