BR112013025549A2 - sais de 2,3-hidroimidazo[1,2-c]quinazolina substituídos - Google Patents
sais de 2,3-hidroimidazo[1,2-c]quinazolina substituídosInfo
- Publication number
- BR112013025549A2 BR112013025549A2 BR112013025549A BR112013025549A BR112013025549A2 BR 112013025549 A2 BR112013025549 A2 BR 112013025549A2 BR 112013025549 A BR112013025549 A BR 112013025549A BR 112013025549 A BR112013025549 A BR 112013025549A BR 112013025549 A2 BR112013025549 A2 BR 112013025549A2
- Authority
- BR
- Brazil
- Prior art keywords
- dihydrochloride salt
- cancer
- prophylaxis
- treatment
- hydroimidazo
- 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
-
- 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
- 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
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)
Abstract
resumo patente de invenção: "sais de 2,3-hidroimidazo[1,2-c]quinazolina substituídos". a presente invenção refere-se: - ao sal de dicloridrato de fórmula 2-amino-n-[7-metóxi-8-(3-morfolin-4-ilpropóxi)-2,3-di-hidroimidazo-[1,2-c]quinazolin-5-il]pirimidina-5-carboxamida (ii): (ii), ou um tautômero, solvato ou hidrato do mesmo ; - aos métodos de preparar referido sal de dicloridrato; - ao referido sal de dicloridrato para o tratamento e/ou profilaxia de uma doença; - ao uso de referido sal de dicloridrato para a preparação de um medicamento para o tratamento e/ou profilaxia de uma doença, em particular de um distúrbio hiperproliferativo e/ou angiogênese, mais particularmente para o tratamento ou profilaxia de um câncer, particularmente câncer de pulmão, em particular carcinoma de pulmão de célula não pequena, câncer colorretal, melanoma, câncer pancreático, carcinoma de hepatócito, câncer pancreático, carcinoma de hepatócito ou câncer de mama; - a uma composição farmacêutica compreendendo o referido sal de dicloridrato; e - a uma combinação farmacêutica compreendendo o referido sal de dicloridrato em combinação com um ou mais outros agentes farmacêuticos.
Applications Claiming Priority (2)
| 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 |
| PCT/EP2012/055600 WO2012136553A1 (en) | 2011-04-05 | 2012-03-29 | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112013025549A2 true BR112013025549A2 (pt) | 2016-12-27 |
Family
ID=43984137
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013025549A BR112013025549A2 (pt) | 2011-04-05 | 2012-03-29 | sais de 2,3-hidroimidazo[1,2-c]quinazolina substituídos |
Country Status (42)
Families Citing this family (33)
| 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 |
| CU24400B1 (es) | 2013-04-08 | 2019-04-04 | Bayer Pharma AG | Una composición que comprende 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas |
| CN105308070A (zh) | 2013-06-14 | 2016-02-03 | 拜耳制药股份公司 | 抗tweakr抗体及其用途 |
| 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 |
| MX2017011635A (es) | 2015-03-09 | 2018-02-09 | Bayer Pharma AG | Combinaciones que contienen 2,3-dihidroimidazo[1,2-c]quinazolina sustituida. |
| 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 |
| LT3274370T (lt) | 2015-03-23 | 2020-02-10 | Bayer Pharma Aktiengesellschaft | Antikūnai prieš ceacam6 ir jų panaudojimas |
| ES2863500T3 (es) | 2015-04-10 | 2021-10-11 | Capsugel Belgium Nv | Formulaciones lipídicas de acetato de abiraterona |
| TN2018000271A1 (en) | 2016-02-01 | 2020-01-16 | Bayer Pharma AG | Copanlisib biomarkers. |
| US20190382839A1 (en) | 2016-02-01 | 2019-12-19 | Bayer Pharma Aktiengesellschaft | Copanlisib biomarkers |
| AU2017225982B2 (en) | 2016-03-02 | 2023-10-05 | Eisai R&D Management Co., Ltd. | Eribulin-based antibody-drug conjugates and methods of use |
| US10844066B2 (en) | 2016-03-08 | 2020-11-24 | 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 |
| EP3515911A1 (en) | 2016-09-23 | 2019-07-31 | Bayer Pharma Aktiengesellschaft | Combination of pi3k-inhibitors |
| CA3045041A1 (en) | 2016-12-14 | 2018-06-21 | 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 |
| CA3068324A1 (en) | 2017-06-28 | 2019-01-03 | Bayer Consumer Care Ag | Combination of a pi3k-inhibitor with an androgen receptor antagonist |
| CU24607B1 (es) | 2017-09-08 | 2022-06-06 | Bayer Consumer Care Ag | Sólido estable, liofilizado, que contiene copanlisib, útil para dilución y aplicaciones terapéuticas |
| EP3498266A1 (en) | 2017-12-15 | 2019-06-19 | Bayer Consumer Care AG | Formulations of copanlisib |
| 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 |
| US20210187134A1 (en) | 2018-08-28 | 2021-06-24 | Bayer As | Combination of pi3k-inhibitors and targeted thorium conjugates |
| CA3116230A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| WO2020079079A1 (en) * | 2018-10-17 | 2020-04-23 | Sandoz Ag | Co-crystals comprising levothyroxine and a dicarboxylic acid |
| US20220064171A1 (en) * | 2018-12-27 | 2022-03-03 | 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 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH588505A5 (pt) | 1972-06-08 | 1977-06-15 | 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 |
| TW225528B (pt) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| 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 |
| JP4790266B2 (ja) | 2002-09-30 | 2011-10-12 | バイエル・シエリング・フアーマ・アクチエンゲゼルシヤフト | 縮合アゾールピリミジン誘導体 |
| 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 |
| 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 |
| PE20091174A1 (es) | 2007-12-27 | 2009-08-03 | Chugai Pharmaceutical Co Ltd | Formulacion liquida con contenido de alta concentracion de anticuerpo |
| 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 |
| EP2168582A1 (en) * | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines |
| HUP0800765A2 (en) | 2008-12-18 | 2010-11-29 | Richter Gedeon Nyrt | A new process for the preparation of piperazine derivatives and their hydrochloric salts |
| EP2558126A2 (en) | 2010-04-16 | 2013-02-20 | Bayer Intellectual Property 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 |
| CU24400B1 (es) | 2013-04-08 | 2019-04-04 | Bayer Pharma AG | Una composición que comprende 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas |
| CN105934256B (zh) | 2013-12-03 | 2019-12-27 | 拜耳制药股份公司 | Pi3k-抑制剂的组合产品 |
| 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 |
| MX2017011635A (es) | 2015-03-09 | 2018-02-09 | Bayer Pharma AG | Combinaciones que contienen 2,3-dihidroimidazo[1,2-c]quinazolina sustituida. |
| 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 |
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2011
- 2011-04-05 EP EP11161111A patent/EP2508525A1/en not_active Withdrawn
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2012
- 2012-03-27 JO JO201264A patent/JO2958B1/en active
- 2012-03-28 AR ARP120101036A patent/AR085718A1/es not_active Application Discontinuation
- 2012-03-28 UY UY0001033985A patent/UY33985A/es not_active Application Discontinuation
- 2012-03-29 SI SI201230138T patent/SI2694508T1/sl unknown
- 2012-03-29 MA MA36288A patent/MA35014B1/fr unknown
- 2012-03-29 AP AP2013007219A patent/AP3709A/en active
- 2012-03-29 ES ES12712104.4T patent/ES2529653T3/es active Active
- 2012-03-29 CA CA2832123A patent/CA2832123C/en active Active
- 2012-03-29 US US14/009,599 patent/US10383876B2/en active Active
- 2012-03-29 EP EP12712104.4A patent/EP2694508B1/en active Active
- 2012-03-29 SG SG2013071501A patent/SG193595A1/en unknown
- 2012-03-29 PE PE2013002186A patent/PE20141038A1/es active IP Right Grant
- 2012-03-29 MX MX2013011583A patent/MX336057B/es unknown
- 2012-03-29 PT PT127121044T patent/PT2694508E/pt unknown
- 2012-03-29 BR BR112013025549A patent/BR112013025549A2/pt not_active Application Discontinuation
- 2012-03-29 ME MEP-2015-16A patent/ME02021B/me unknown
- 2012-03-29 PL PL12712104T patent/PL2694508T3/pl unknown
- 2012-03-29 MY MYPI2013701860A patent/MY169452A/en unknown
- 2012-03-29 EA EA201391470A patent/EA023646B1/ru not_active IP Right Cessation
- 2012-03-29 UA UAA201312858A patent/UA111604C2/uk unknown
- 2012-03-29 CU CUP2013000133A patent/CU24208B1/es active IP Right Grant
- 2012-03-29 AU AU2012238891A patent/AU2012238891B2/en active Active
- 2012-03-29 KR KR1020137028852A patent/KR101937501B1/ko active IP Right Grant
- 2012-03-29 DK DK12712104.4T patent/DK2694508T3/en active
- 2012-03-29 CN CN201280027509.4A patent/CN103649091B/zh active Active
- 2012-03-29 RS RS20150077A patent/RS53811B1/en unknown
- 2012-03-29 JP JP2014503079A patent/JP5763834B2/ja active Active
- 2012-03-29 WO PCT/EP2012/055600 patent/WO2012136553A1/en active Application Filing
- 2012-03-30 TW TW105122778A patent/TWI592158B/zh active
- 2012-03-30 TW TW101111580A patent/TWI549954B/zh active
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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 CR CR20130511A patent/CR20130511A/es unknown
- 2013-10-04 CL CL2013002870A patent/CL2013002870A1/es unknown
- 2013-10-04 CO CO13236625A patent/CO6781534A2/es not_active Application Discontinuation
- 2013-10-04 GT GT201300234A patent/GT201300234A/es unknown
- 2013-10-04 DO DO2013000223A patent/DOP2013000223A/es unknown
- 2013-11-04 EC ECSP13013006 patent/ECSP13013006A/es unknown
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2014
- 2014-09-16 HK HK14109333.1A patent/HK1195907A1/zh unknown
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2015
- 2015-02-04 HR HRP20150138TT patent/HRP20150138T1/hr unknown
- 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 active Active
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2016
- 2016-01-07 US US14/990,350 patent/US9636344B2/en active Active
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