BR112017019188A2 - Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas - Google Patents

Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas

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Publication number
BR112017019188A2
BR112017019188A2 BR112017019188-1A BR112017019188A BR112017019188A2 BR 112017019188 A2 BR112017019188 A2 BR 112017019188A2 BR 112017019188 A BR112017019188 A BR 112017019188A BR 112017019188 A2 BR112017019188 A2 BR 112017019188A2
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BR
Brazil
Prior art keywords
pten
loss
quinazoline
combinations
pik3r5
Prior art date
Application number
BR112017019188-1A
Other languages
English (en)
Inventor
Liu Ningshu
Pena Carol
Jeffers Michael
GENVRESSE Isabelle
Original Assignee
Bayer Pharma Aktiengesellschaft
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Publication date
Application filed by Bayer Pharma Aktiengesellschaft filed Critical Bayer Pharma Aktiengesellschaft
Publication of BR112017019188A2 publication Critical patent/BR112017019188A2/pt

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    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/156—Polymorphic or mutational markers
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/158—Expression markers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Analytical Chemistry (AREA)
  • Wood Science & Technology (AREA)
  • Immunology (AREA)
  • Pathology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

?combinações contendo 2,3-di-hidroimidazo[1,2-c]quinazolina substituídas? a presente invenção refere-se a: * combinações de: componente a: um ou mais compostos de 2,3-di-hidroimidazo[1,2-c]quinazolina da fórmula geral (a1) ou (a2), ou um sal fisiologicamente aceitável, solvato, hidrato ou estereoisômero deste; componente b: um ou mais compostos substituídos de 5-(1-benzotiofen-2-il)pirrolo[2,1-f][1,2,4]-triazin-4-amina da fórmula geral (b), ou um sal fisiologicamente aceitável, solvato, hidrato ou estereoisômero deste; em que opcionalmente alguns ou todos os componentes estão na forma de uma formulação farmacêutica pronta para uso para ser administrada simultaneamente, concomitantemente, separadamente ou sequencialmente. dependentemente entre si pelas vias oral, intravenosa, tópica, instalações locais, via intraperitoneal ou nasal; * uso das ditas combinações para a preparação de um medicamento para o tratamento ou profilaxia de um câncer; * um kit compreendendo a dita combinação; * uso de biomarcadores que é a perda do supressor tumoral pten ou fbxw7, para prever a sensibilidade e/ou a resistência de um paciente com câncer ao dito composto e para prover uma dosagem com base em justificativa para aumentar a sensibilidade e/ou para superar a resistência; * um método para determinar a perda do supressor tumoral pten ou fbxw7; e * um método para determinar perturbações em pik3ca, pik3cb, pik3cd, pik3cg, pik3r1, pik3r2, pik3r3, pik3r4, pik3r5, fgfr1, fgfr2, fgfr3 e/ou fgfr4; perda de pten e alteração de pik3ca, pik3cb, pik3cd, pik3cg, pik3r1, pik3r2, pik3r3, pik3r4, pik3r5, fgfr1, fgfr2, fgfr3 e/ou fgfr4.
BR112017019188-1A 2015-03-09 2016-03-07 Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas BR112017019188A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562130418P 2015-03-09 2015-03-09
US62/130,418 2015-03-09
PCT/EP2016/054727 WO2016142312A1 (en) 2015-03-09 2016-03-07 Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations

Publications (1)

Publication Number Publication Date
BR112017019188A2 true BR112017019188A2 (pt) 2018-04-24

Family

ID=55538186

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017019188-1A BR112017019188A2 (pt) 2015-03-09 2016-03-07 Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas

Country Status (15)

Country Link
US (1) US10406162B2 (pt)
EP (1) EP3268490B1 (pt)
JP (1) JP6867295B2 (pt)
KR (1) KR20180013851A (pt)
CN (1) CN107864625B (pt)
AU (1) AU2016231259A1 (pt)
BR (1) BR112017019188A2 (pt)
CA (1) CA2978830A1 (pt)
EA (1) EA201791974A1 (pt)
IL (1) IL254167A0 (pt)
MX (1) MX2017011635A (pt)
PH (1) PH12017501643A1 (pt)
SG (1) SG11201707240SA (pt)
SV (1) SV2017005530A (pt)
WO (1) WO2016142312A1 (pt)

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* Cited by examiner, † Cited by third party
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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
ES2708350T3 (es) 2013-04-08 2019-04-09 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas para el tratamiento de linfomas
EP3018127A1 (en) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
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
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
WO2018054782A1 (en) 2016-09-23 2018-03-29 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors
CN111032662B (zh) 2017-06-21 2024-10-15 尚医治疗有限责任公司 与ras超家族相互作用的用于治疗癌症、炎性疾病、ras蛋白病和纤维化疾病的化合物
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WO2019105734A1 (en) * 2017-11-28 2019-06-06 Bayer Consumer Care Ag Combinations of copanlisib
CN111500587A (zh) * 2020-04-15 2020-08-07 湖南省科域生物医药科技有限公司 Pgr作为治疗子宫内膜异位症的产品中的用途及其检测pgr的试剂盒

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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
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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
BR112012026480A2 (pt) * 2010-04-16 2016-08-16 Bayer Ip Gmbh combinações contendo 2,3-di-hidroimidazo[1,2-c]quinazolina substituída
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
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EP3018131A1 (en) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
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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
JOP20210204A1 (ar) * 2019-01-31 2023-01-30 Bayer Ag أحادي هيدرات هيدروكلوريد روجاراتينيب وأشكال صلبة منه

Also Published As

Publication number Publication date
SV2017005530A (es) 2018-10-02
EA201791974A1 (ru) 2018-05-31
IL254167A0 (en) 2017-10-31
SG11201707240SA (en) 2017-10-30
EP3268490A1 (en) 2018-01-17
KR20180013851A (ko) 2018-02-07
CN107864625B (zh) 2021-05-28
AU2016231259A1 (en) 2017-09-21
CA2978830A1 (en) 2016-09-15
MX2017011635A (es) 2018-02-09
US10406162B2 (en) 2019-09-10
PH12017501643A1 (en) 2018-03-12
JP6867295B2 (ja) 2021-04-28
WO2016142312A1 (en) 2016-09-15
EP3268490B1 (en) 2020-07-08
US20180055851A1 (en) 2018-03-01
JP2018510869A (ja) 2018-04-19
CN107864625A (zh) 2018-03-30

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