DOP2017000112A - Síntesis de copanlisib y su sal diclorhidrato - Google Patents
Síntesis de copanlisib y su sal diclorhidratoInfo
- Publication number
- DOP2017000112A DOP2017000112A DO2017000112A DO2017000112A DOP2017000112A DO P2017000112 A DOP2017000112 A DO P2017000112A DO 2017000112 A DO2017000112 A DO 2017000112A DO 2017000112 A DO2017000112 A DO 2017000112A DO P2017000112 A DOP2017000112 A DO P2017000112A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- copanlisib
- diclorhydrate
- synthesis
- salt
- dihydrochloride
- 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
Abstract
La presente invención se relaciona con un nuevo método para preparar copanlisib, diclorhidrato de copanlisib, o hidratos de diclorhidrato de copanlisib, con nuevos compuestos intermediarios, y con el uso de dichos nuevos compuestos intermediarios en la preparación de copanlisib, diclorhidrato de copanlisib, o hidratos de diclorhidrato de copanlisib. La presente invención también se relaciona con hidratos de diclorhidrato de copanlisib como compuestos.
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 |
|---|---|
| DOP2017000112A true DOP2017000112A (es) | 2017-06-15 |
Family
ID=51866061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DO2017000112A DOP2017000112A (es) | 2014-11-07 | 2017-05-05 | Síntesis 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 |
| CA2908776C (en) | 2013-04-08 | 2021-08-10 | Bayer Pharma Aktiengesellschaft | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas |
| MX2017011635A (es) | 2015-03-09 | 2018-02-09 | Bayer Pharma AG | Combinaciones que contienen 2,3-dihidroimidazo[1,2-c]quinazolina sustituida. |
| 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 |
| 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 |
| 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 |
| MX2020002633A (es) | 2017-09-08 | 2020-07-13 | Bayer Consumer Care Ag | Formulaciones de 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 |
| ES2367141T3 (es) | 2002-09-30 | 2011-10-28 | Bayer Pharma Aktiengesellschaft | Derivados de azol-pirimidina condensados. |
| 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 |
| WO2009091550A2 (en) * | 2008-01-14 | 2009-07-23 | Bayer Healthcare Llc | 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 |
| CA2908776C (en) | 2013-04-08 | 2021-08-10 | Bayer Pharma Aktiengesellschaft | 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 |
| MX2017011635A (es) | 2015-03-09 | 2018-02-09 | Bayer Pharma AG | Combinaciones que contienen 2,3-dihidroimidazo[1,2-c]quinazolina sustituida. |
| MA43840A (fr) | 2015-03-09 | 2018-11-21 | Bayer Healthcare Pharmaceuticals Inc | Utilisation de 2,3-dihydroimidazo[1,2-c]quinazolines substituées |
| TN2018000272A1 (en) | 2016-02-01 | 2020-01-16 | Bayer Pharma AG | Copanlisib biomarkers |
| EP3411497A1 (en) | 2016-02-01 | 2018-12-12 | 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 |
| 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 |
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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 ME MEP-2019-107A patent/ME03358B/me unknown
- 2015-11-05 NZ NZ731287A patent/NZ731287A/en unknown
- 2015-11-05 AU AU2015341788A patent/AU2015341788B2/en active Active
- 2015-11-05 UA UAA201705433A patent/UA122398C2/uk unknown
- 2015-11-05 MX MX2017005893A patent/MX366904B/es active IP Right Grant
- 2015-11-05 EP EP15790150.5A patent/EP3215493B1/en active Active
- 2015-11-05 CA CA2966800A patent/CA2966800C/en active Active
- 2015-11-05 PL PL15790150T patent/PL3215493T3/pl unknown
- 2015-11-05 MY MYPI2017701550A patent/MY189852A/en unknown
- 2015-11-05 US US15/524,581 patent/US10494372B2/en active Active
- 2015-11-05 MA MA40895A patent/MA40895B1/fr unknown
- 2015-11-05 BR BR112017009470-3A patent/BR112017009470B1/pt active IP Right Grant
- 2015-11-05 TR TR2019/05217T patent/TR201905217T4/tr unknown
- 2015-11-05 CU CU2017000061A patent/CU24489B1/es unknown
- 2015-11-05 UY UY0001036392A patent/UY36392A/es not_active Application Discontinuation
- 2015-11-05 RS RS20190453A patent/RS58579B1/sr unknown
- 2015-11-05 CR CR20170184A patent/CR20170184A/es unknown
- 2015-11-05 ES ES15790150T patent/ES2721778T3/es active Active
- 2015-11-05 PE PE2017000818A patent/PE20170897A1/es unknown
- 2015-11-05 PT PT15790150T patent/PT3215493T/pt unknown
- 2015-11-05 LT LTEP15790150.5T patent/LT3215493T/lt unknown
- 2015-11-05 HU HUE15790150A patent/HUE042866T2/hu unknown
- 2015-11-05 EA EA201790983A patent/EA035558B1/ru not_active IP Right Cessation
- 2015-11-05 JP JP2017523881A patent/JP6691115B2/ja active Active
- 2015-11-05 DK DK15790150.5T patent/DK3215493T3/da 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 KR KR1020177014992A patent/KR102566834B1/ko active IP Right Grant
- 2015-11-05 SG SG11201703702RA patent/SG11201703702RA/en unknown
- 2015-11-05 CN CN201580072735.8A patent/CN107278204B/zh active Active
- 2015-11-05 SI SI201530695T patent/SI3215493T1/sl unknown
- 2015-11-06 TW TW104136742A patent/TWI697495B/zh active
- 2015-11-06 AR ARP150103619A patent/AR102570A1/es unknown
-
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 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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