PE20170897A1 - Sintesis de copanlisib y su sal diclorhidrato - Google Patents
Sintesis de copanlisib y su sal diclorhidratoInfo
- Publication number
- PE20170897A1 PE20170897A1 PE2017000818A PE2017000818A PE20170897A1 PE 20170897 A1 PE20170897 A1 PE 20170897A1 PE 2017000818 A PE2017000818 A PE 2017000818A PE 2017000818 A PE2017000818 A PE 2017000818A PE 20170897 A1 PE20170897 A1 PE 20170897A1
- Authority
- PE
- Peru
- Prior art keywords
- copanlisib
- optionally
- 2theta
- xrpd
- copper
- Prior art date
Links
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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se refiere a un metodo para preparar 2-amino-N-[7-metoxi-8-(3-morfolin-4-ilpropoxi)-2,3-dihidroimidazo-[1,2-c]quinazolin-5-il]pirimidin-5-carboxamida (copanlisib) de formula (1), que comprende reaccionar el compuesto a) con b) opcionalmente en presencia de un catalizador, tal como N, N-dimetil-4-aminopiridina, opcionalmente en presencia de un agente de acoplamiento tal como clorhidrato de N- [3-(dimetilamino)propil]-N´-etilcarbodiimida, opcionalmente en un solvente, tal como N, N-dimetilformamida; Son sales de diclorhidrato selectivos: diclorhidrato de copanlisib hidrato I de un pico maximo de XRPD [°2theta] (Cobre (Cu)) de 5,6; diclorhidrato de copanlisib hidrato II de un pico maximo de XRPD [°2theta] (Cobre (Cu)) de 5,7; entre otros. Dicho compuesto inhibe las fosfatidilinositol-3-quinasas de clase I siendo util como anticancerigeno
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 |
|---|---|
| PE20170897A1 true PE20170897A1 (es) | 2017-07-12 |
Family
ID=51866061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000818A PE20170897A1 (es) | 2014-11-07 | 2015-11-05 | Sintesis de copanlisib y su sal diclorhidrato |
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 |
| SG10201710539QA (en) | 2013-04-08 | 2018-01-30 | Bayer Pharma AG | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas |
| BR112017019188A2 (pt) | 2015-03-09 | 2018-04-24 | Bayer Pharma Aktiengesellschaft | Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas |
| 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 |
| 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 |
| US11185549B2 (en) | 2017-06-28 | 2021-11-30 | Bayer Consumer Care Ag | Combination of a PI3K-inhibitor with an androgen receptor antagonist |
| PL3678644T3 (pl) | 2017-09-08 | 2023-09-11 | Bayer Pharma Aktiengesellschaft | Formulacje kopanlizybu |
| 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 |
| 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 |
| 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 |
| EP2244721A4 (en) * | 2008-01-14 | 2017-01-18 | Bayer Intellectual Property GmbH | Sulfone substituted 2,3-dihydroimidazo ý1,2-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 |
| 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 |
| SG10201710539QA (en) | 2013-04-08 | 2018-01-30 | Bayer Pharma AG | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas |
| 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 |
| BR112017019188A2 (pt) | 2015-03-09 | 2018-04-24 | Bayer Pharma Aktiengesellschaft | Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas |
| TN2017000385A1 (en) | 2015-03-09 | 2019-01-16 | Bayer Healthcare Pharmaceuticals Inc | Use of substituted 2,3-dihydroimidaz0[1,2-c]quinazolines. |
| CA3012951A1 (en) | 2016-02-01 | 2017-08-10 | Bayer Pharma Aktiengesellschaft | Copanlisib biomarkers |
| AU2017214230A1 (en) | 2016-02-01 | 2018-08-09 | Bayer Pharma Aktiengesellschaft | 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 |
| CA3037626A1 (en) | 2016-09-23 | 2018-03-29 | Bayer Pharma Aktiengesellschaft | Combination of pi3k-inhibitors |
-
2014
- 2014-11-07 EP EP14192203.9A patent/EP3018127A1/en not_active Withdrawn
-
2015
- 2015-11-04 JO JOP/2015/0274A patent/JO3644B1/ar active
- 2015-11-05 SI SI201530695T patent/SI3215493T1/sl 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 TR TR2019/05217T patent/TR201905217T4/tr unknown
- 2015-11-05 CU CU2017000061A patent/CU24489B1/es unknown
- 2015-11-05 AU AU2015341788A patent/AU2015341788B2/en active Active
- 2015-11-05 TN TN2017000179A patent/TN2017000179A1/en unknown
- 2015-11-05 WO PCT/EP2015/075789 patent/WO2016071435A2/en active Application Filing
- 2015-11-05 UA UAA201705433A patent/UA122398C2/uk unknown
- 2015-11-05 EP EP15790150.5A patent/EP3215493B1/en active Active
- 2015-11-05 MX MX2017005893A patent/MX366904B/es active IP Right Grant
- 2015-11-05 HU HUE15790150A patent/HUE042866T2/hu unknown
- 2015-11-05 PL PL15790150T patent/PL3215493T3/pl unknown
- 2015-11-05 JP JP2017523881A patent/JP6691115B2/ja active Active
- 2015-11-05 CR CR20170184A patent/CR20170184A/es unknown
- 2015-11-05 CN CN201580072735.8A patent/CN107278204B/zh active Active
- 2015-11-05 ES ES15790150T patent/ES2721778T3/es active Active
- 2015-11-05 PT PT15790150T patent/PT3215493T/pt unknown
- 2015-11-05 DK DK15790150.5T patent/DK3215493T3/da active
- 2015-11-05 UY UY0001036392A patent/UY36392A/es not_active Application Discontinuation
- 2015-11-05 NZ NZ731287A patent/NZ731287A/en unknown
- 2015-11-05 PE PE2017000818A patent/PE20170897A1/es unknown
- 2015-11-05 RS RS20190453A patent/RS58579B1/sr unknown
- 2015-11-05 MA MA40895A patent/MA40895B1/fr unknown
- 2015-11-05 KR KR1020177014992A patent/KR102566834B1/ko active IP Right Grant
- 2015-11-05 ME MEP-2019-107A patent/ME03358B/me unknown
- 2015-11-05 BR BR112017009470-3A patent/BR112017009470B1/pt active IP Right Grant
- 2015-11-05 MY MYPI2017701550A patent/MY189852A/en unknown
- 2015-11-05 SG SG11201703702RA patent/SG11201703702RA/en unknown
- 2015-11-05 US US15/524,581 patent/US10494372B2/en active Active
- 2015-11-05 CA CA2966800A patent/CA2966800C/en active Active
- 2015-11-06 AR ARP150103619A patent/AR102570A1/es unknown
- 2015-11-06 TW TW104136742A patent/TWI697495B/zh active
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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 SV SV2017005433A patent/SV2017005433A/es unknown
- 2017-05-05 DO DO2017000112A patent/DOP2017000112A/es unknown
- 2017-05-05 CO CONC2017/0004532A patent/CO2017004532A2/es unknown
- 2017-05-05 NI NI201700054A patent/NI201700054A/es unknown
- 2017-05-05 EC ECIEPI201727755A patent/ECSP17027755A/es unknown
- 2017-05-05 CL CL2017001131A patent/CL2017001131A1/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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