EA201790983A1 - Синтез копанлисиба и его дигидрохлорида - Google Patents
Синтез копанлисиба и его дигидрохлоридаInfo
- Publication number
- EA201790983A1 EA201790983A1 EA201790983A EA201790983A EA201790983A1 EA 201790983 A1 EA201790983 A1 EA 201790983A1 EA 201790983 A EA201790983 A EA 201790983A EA 201790983 A EA201790983 A EA 201790983A EA 201790983 A1 EA201790983 A1 EA 201790983A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- dihydrochloride
- copanlisib
- kopanlisib
- synthesis
- hydrates
- Prior art date
Links
Classifications
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- 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
Настоящее изобретение относится к новому способу получения копанлисиба, дигидрохлорида копанлисиба, или гидратов дигидрохлорида копанлисиба, к новым промежуточным соединениям и к применению указанных новых промежуточных соединений для приготовления указанного копанлисиба, дигидрохлорида копанлисиба, или гидратов дигидрохлорида копанлисиба. Настоящее изобретение также относится к гидратам дигидрохлорида копанлисиба в качестве соединений.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14192203.9A EP3018127A1 (en) | 2014-11-07 | 2014-11-07 | Synthesis of copanlisib and its dihydrochloride salt |
| PCT/EP2015/075789 WO2016071435A2 (en) | 2014-11-07 | 2015-11-05 | Synthesis of copanlisib and its dihydrochloride salt |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201790983A1 true EA201790983A1 (ru) | 2017-10-31 |
| EA035558B1 EA035558B1 (ru) | 2020-07-07 |
Family
ID=51866061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201790983A EA035558B1 (ru) | 2014-11-07 | 2015-11-05 | Синтез копанлисиба и его дигидрохлорида |
Country Status (47)
Families Citing this family (12)
| 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 |
| TN2015000452A1 (en) | 2013-04-08 | 2017-04-06 | Bayer Pharma AG | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas |
| WO2016142312A1 (en) | 2015-03-09 | 2016-09-15 | Bayer Pharma Aktiengesellschaft | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations |
| 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 |
| JP2019532922A (ja) | 2016-09-23 | 2019-11-14 | 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 |
| 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 |
| RS64316B1 (sr) | 2017-09-08 | 2023-08-31 | Bayer Pharma AG | Formulacije kopanlisiba |
| EP3498266A1 (en) | 2017-12-15 | 2019-06-19 | Bayer Consumer Care AG | Formulations of copanlisib |
| 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 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1003580A (en) | 1910-08-10 | 1911-09-19 | Remington Typewriter Co | Type-writing machine. |
| 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 |
| JP4445751B2 (ja) * | 2001-08-15 | 2010-04-07 | イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー | 無脊椎有害生物を防除するためのｏ−複素環式置換アリールアミド |
| SI1549652T1 (sl) | 2002-09-30 | 2009-04-30 | Bayer Healthcare Ag | Kondenzirani azolpirimidinski derivati |
| 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 |
| US8859572B2 (en) | 2008-01-14 | 2014-10-14 | Bayer Intellectual Property Gmbh | Sulfone substituted 2,3-dihydroimidazo [1,2-C] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis |
| 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 |
| TN2015000452A1 (en) | 2013-04-08 | 2017-04-06 | Bayer Pharma AG | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas |
| US10117874B2 (en) | 2013-12-03 | 2018-11-06 | 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 |
| BR112017019190A2 (pt) | 2015-03-09 | 2018-04-24 | Bayer Healthcare Pharmaceuticals Inc | uso de 2,3-di-hidroimidazo[1,2-c]quinazolinas substituídas |
| WO2016142312A1 (en) | 2015-03-09 | 2016-09-15 | Bayer Pharma Aktiengesellschaft | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations |
| KR20180104129A (ko) | 2016-02-01 | 2018-09-19 | 바이엘 파마 악티엔게젤샤프트 | 코판리십 바이오마커 |
| SG10202007262PA (en) | 2016-02-01 | 2020-09-29 | Bayer Pharma AG | Copanlisib biomarkers |
| 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 |
| JP2019532922A (ja) | 2016-09-23 | 2019-11-14 | 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 |
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2014
- 2014-11-07 EP EP14192203.9A patent/EP3018127A1/en not_active Withdrawn
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2015
- 2015-11-04 JO JOP/2015/0274A patent/JO3644B1/ar active
- 2015-11-05 US US15/524,581 patent/US10494372B2/en active Active
- 2015-11-05 PT PT15790150T patent/PT3215493T/pt unknown
- 2015-11-05 PE PE2017000818A patent/PE20170897A1/es unknown
- 2015-11-05 SI SI201530695T patent/SI3215493T1/sl unknown
- 2015-11-05 CN CN201580072735.8A patent/CN107278204B/zh active Active
- 2015-11-05 DK DK15790150.5T patent/DK3215493T3/da active
- 2015-11-05 AU AU2015341788A patent/AU2015341788B2/en active Active
- 2015-11-05 MX MX2017005893A patent/MX366904B/es active IP Right Grant
- 2015-11-05 KR KR1020177014992A patent/KR102566834B1/ko active IP Right Grant
- 2015-11-05 SG SG11201703702RA patent/SG11201703702RA/en unknown
- 2015-11-05 CU CU2017000061A patent/CU24489B1/es unknown
- 2015-11-05 CA CA2966800A patent/CA2966800C/en active Active
- 2015-11-05 MY MYPI2017701550A patent/MY189852A/en unknown
- 2015-11-05 UA UAA201705433A patent/UA122398C2/uk unknown
- 2015-11-05 HU HUE15790150A patent/HUE042866T2/hu unknown
- 2015-11-05 CR CR20170184A patent/CR20170184A/es unknown
- 2015-11-05 LT LTEP15790150.5T patent/LT3215493T/lt unknown
- 2015-11-05 EA EA201790983A patent/EA035558B1/ru not_active IP Right Cessation
- 2015-11-05 NZ NZ731287A patent/NZ731287A/en unknown
- 2015-11-05 MA MA40895A patent/MA40895B1/fr unknown
- 2015-11-05 JP JP2017523881A patent/JP6691115B2/ja active Active
- 2015-11-05 TR TR2019/05217T patent/TR201905217T4/tr unknown
- 2015-11-05 TN TN2017000179A patent/TN2017000179A1/en unknown
- 2015-11-05 RS RS20190453A patent/RS58579B1/sr unknown
- 2015-11-05 ME MEP-2019-107A patent/ME03358B/me unknown
- 2015-11-05 UY UY0001036392A patent/UY36392A/es not_active Application Discontinuation
- 2015-11-05 PL PL15790150T patent/PL3215493T3/pl unknown
- 2015-11-05 ES ES15790150T patent/ES2721778T3/es active Active
- 2015-11-05 EP EP15790150.5A patent/EP3215493B1/en active Active
- 2015-11-05 WO PCT/EP2015/075789 patent/WO2016071435A2/en active Application Filing
- 2015-11-05 BR BR112017009470-3A patent/BR112017009470B1/pt active IP Right Grant
- 2015-11-06 TW TW104136742A patent/TWI697495B/zh active
- 2015-11-06 AR ARP150103619A patent/AR102570A1/es unknown
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2017
- 2017-04-24 IL IL251874A patent/IL251874A0/en active IP Right Grant
- 2017-05-04 SA SA517381462A patent/SA517381462B1/ar unknown
- 2017-05-04 PH PH12017500833A patent/PH12017500833A1/en unknown
- 2017-05-05 DO DO2017000112A patent/DOP2017000112A/es unknown
- 2017-05-05 SV SV2017005433A patent/SV2017005433A/es unknown
- 2017-05-05 CL CL2017001131A patent/CL2017001131A1/es unknown
- 2017-05-05 EC ECIEPI201727755A patent/ECSP17027755A/es unknown
- 2017-05-05 NI NI201700054A patent/NI201700054A/es unknown
- 2017-05-05 CO CONC2017/0004532A patent/CO2017004532A2/es unknown
- 2017-06-06 ZA ZA2017/03867A patent/ZA201703867B/en unknown
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2018
- 2018-04-19 HK HK18105077.5A patent/HK1245774A1/zh unknown
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2019
- 2019-04-16 HR HRP20190720TT patent/HRP20190720T1/hr unknown
- 2019-04-23 CY CY20191100444T patent/CY1121602T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AZ KG TJ TM |