TWI549954B - 經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽 - Google Patents
經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽 Download PDFInfo
- Publication number
- TWI549954B TWI549954B TW101111580A TW101111580A TWI549954B TW I549954 B TWI549954 B TW I549954B TW 101111580 A TW101111580 A TW 101111580A TW 101111580 A TW101111580 A TW 101111580A TW I549954 B TWI549954 B TW I549954B
- Authority
- TW
- Taiwan
- Prior art keywords
- formula
- hours
- cancer
- salt
- acid
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- 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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11161111A EP2508525A1 (en) | 2011-04-05 | 2011-04-05 | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201249847A TW201249847A (en) | 2012-12-16 |
| TWI549954B true TWI549954B (zh) | 2016-09-21 |
Family
ID=43984137
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW101111580A TWI549954B (zh) | 2011-04-05 | 2012-03-30 | 經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽 |
| TW105122778A TWI592158B (zh) | 2011-04-05 | 2012-03-30 | 經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW105122778A TWI592158B (zh) | 2011-04-05 | 2012-03-30 | 經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽 |
Country Status (42)
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| WO2023218032A1 (en) | 2022-05-13 | 2023-11-16 | Synthon B.V. | Solid forms of copanlisib salts |
| WO2025053315A1 (ko) * | 2023-09-08 | 2025-03-13 | 파로스젠 주식회사 | 항암제 프로드러그 컨쥬게이트의 제조에서 팔라듐의 회수 및 제거 방법 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101631464A (zh) * | 2006-12-05 | 2010-01-20 | 拜耳先灵医药股份有限公司 | 用于治疗过度增殖疾病和血管发生相关性疾病的2,3-二氢咪唑并[1,2-c]喹唑啉取代衍生物 |
| EP2168582A1 (en) * | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH605550A5 (https=) | 1972-06-08 | 1978-09-29 | Research Corp | |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (https=) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| GB0021865D0 (en) | 2000-09-06 | 2000-10-18 | Smithkline Beecham Plc | Novel pharmaceutical |
| UA82205C2 (en) * | 2002-09-30 | 2008-03-25 | Байер Фармасьютикалз Корпорейшн | Fused azole-pyrimidine derivatives |
| JP4323793B2 (ja) | 2002-12-16 | 2009-09-02 | キヤノン株式会社 | ズームレンズ及びそれを有する光学機器 |
| PE20091174A1 (es) | 2007-12-27 | 2009-08-03 | Chugai Pharmaceutical Co Ltd | Formulacion liquida con contenido de alta concentracion de anticuerpo |
| CA2713388C (en) * | 2008-01-14 | 2016-03-29 | William Scott | Sulfone substituted 2,3-dihydroimidazo [1,2-c] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated 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 |
| HUP0800765A2 (en) | 2008-12-18 | 2010-11-29 | Richter Gedeon Nyrt | A new process for the preparation of piperazine derivatives and their hydrochloric salts |
| PH12012502069A1 (en) | 2010-04-16 | 2013-02-04 | Bayer Ip Gmbh | Substituted 2,3-dihydroimidazo [1,2-c] quinazoline - containing combinations |
| UA113280C2 (xx) | 2010-11-11 | 2017-01-10 | АМІНОСПИРТЗАМІЩЕНІ ПОХІДНІ 2,3-ДИГІДРОІМІДАЗО$1,2-c]ХІНАЗОЛІНУ, ПРИДАТНІ ДЛЯ ЛІКУВАННЯ ГІПЕРПРОЛІФЕРАТИВНИХ ПОРУШЕНЬ І ЗАХВОРЮВАНЬ, ПОВ'ЯЗАНИХ З АНГІОГЕНЕЗОМ | |
| 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 |
| 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 |
-
2011
- 2011-04-05 EP EP11161111A patent/EP2508525A1/en not_active Withdrawn
-
2012
- 2012-03-27 JO JO201264A patent/JO2958B1/en active
- 2012-03-28 UY UY0001033985A patent/UY33985A/es not_active Application Discontinuation
- 2012-03-28 AR ARP120101036A patent/AR085718A1/es not_active Application Discontinuation
- 2012-03-29 SG SG2013071501A patent/SG193595A1/en unknown
- 2012-03-29 CA CA2832123A patent/CA2832123C/en active Active
- 2012-03-29 AU AU2012238891A patent/AU2012238891B2/en not_active Ceased
- 2012-03-29 EP EP12712104.4A patent/EP2694508B1/en active Active
- 2012-03-29 RS RS20150077A patent/RS53811B1/sr unknown
- 2012-03-29 PT PT127121044T patent/PT2694508E/pt unknown
- 2012-03-29 HR HRP20150138TT patent/HRP20150138T1/hr unknown
- 2012-03-29 US US14/009,599 patent/US10383876B2/en active Active
- 2012-03-29 CN CN201280027509.4A patent/CN103649091B/zh not_active Expired - Fee Related
- 2012-03-29 MY MYPI2013701860A patent/MY169452A/en unknown
- 2012-03-29 PE PE2013002186A patent/PE20141038A1/es active IP Right Grant
- 2012-03-29 SI SI201230138T patent/SI2694508T1/sl unknown
- 2012-03-29 UA UAA201312858A patent/UA111604C2/uk unknown
- 2012-03-29 ES ES12712104.4T patent/ES2529653T3/es active Active
- 2012-03-29 ME MEP-2015-16A patent/ME02021B/me unknown
- 2012-03-29 MX MX2013011583A patent/MX336057B/es unknown
- 2012-03-29 PL PL12712104T patent/PL2694508T3/pl unknown
- 2012-03-29 MA MA36288A patent/MA35014B1/fr unknown
- 2012-03-29 BR BR112013025549A patent/BR112013025549A2/pt not_active Application Discontinuation
- 2012-03-29 JP JP2014503079A patent/JP5763834B2/ja not_active Expired - Fee Related
- 2012-03-29 PH PH1/2013/502065A patent/PH12013502065A1/en unknown
- 2012-03-29 KR KR1020137028852A patent/KR101937501B1/ko not_active Expired - Fee Related
- 2012-03-29 AP AP2013007219A patent/AP3709A/en active
- 2012-03-29 CU CUP2013000133A patent/CU24208B1/es active IP Right Grant
- 2012-03-29 EA EA201391470A patent/EA023646B1/ru not_active IP Right Cessation
- 2012-03-29 DK DK12712104.4T patent/DK2694508T3/en active
- 2012-03-29 WO PCT/EP2012/055600 patent/WO2012136553A1/en not_active Ceased
- 2012-03-30 TW TW101111580A patent/TWI549954B/zh not_active IP Right Cessation
- 2012-03-30 TW TW105122778A patent/TWI592158B/zh not_active IP Right Cessation
-
2013
- 2013-09-20 ZA ZA2013/07105A patent/ZA201307105B/en unknown
- 2013-09-29 IL IL228561A patent/IL228561A/en active IP Right Grant
- 2013-10-03 TN TNP2013000401A patent/TN2013000401A1/fr unknown
- 2013-10-04 GT GT201300234A patent/GT201300234A/es unknown
- 2013-10-04 CO CO13236625A patent/CO6781534A2/es not_active Application Discontinuation
- 2013-10-04 CL CL2013002870A patent/CL2013002870A1/es unknown
- 2013-10-04 DO DO2013000223A patent/DOP2013000223A/es unknown
- 2013-10-04 CR CR20130511A patent/CR20130511A/es unknown
- 2013-11-04 EC ECSP13013006 patent/ECSP13013006A/es unknown
-
2015
- 2015-02-12 SM SM201500037T patent/SMT201500037B/xx unknown
- 2015-02-19 CY CY20151100174T patent/CY1116231T1/el unknown
- 2015-04-28 JP JP2015091455A patent/JP5826961B2/ja not_active Expired - Fee Related
-
2016
- 2016-01-07 US US14/990,350 patent/US9636344B2/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101631464A (zh) * | 2006-12-05 | 2010-01-20 | 拜耳先灵医药股份有限公司 | 用于治疗过度增殖疾病和血管发生相关性疾病的2,3-二氢咪唑并[1,2-c]喹唑啉取代衍生物 |
| EP2168582A1 (en) * | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI549954B (zh) | 經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽 | |
| AU2009286982B2 (en) | N-(2-aminophenyl)-4-[N-(pyridine-3-yl)-methoxycarbonyl-aminomethyl]-benzamide (MS-275)polymorph B | |
| TW201437211A (zh) | 經取代咪唑并嗒□ | |
| JP2018512403A (ja) | 置換２，３−ジヒドロイミダゾ［１，２−ｃ］キナゾリン類の使用 | |
| CN107108636A (zh) | 6‑羟基苯并呋喃基‑和6‑烷氧基苯并呋喃基‑取代的咪唑并哒嗪 | |
| NZ616198B2 (en) | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts | |
| HK1195907B (en) | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts | |
| US20160045496A1 (en) | Use of (rs)-s-cyclopropyl-s-(4--5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide for treatment of specific tumours | |
| HK1239665A1 (en) | 6-hydroxybenzofuranyl- and 6-alkoxybenzofuranyl-substituted imidazopyridazines | |
| HK1179529A (en) | Use of novel pan-cdk inhibitors for treating tumors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Annulment or lapse of patent due to non-payment of fees |