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RU2013154355A - Способ лечения мезотелиомы ингибитором рi3к - Google Patents

Способ лечения мезотелиомы ингибитором рi3к Download PDF

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RU2013154355A
RU2013154355A RU2013154355/15A RU2013154355A RU2013154355A RU 2013154355 A RU2013154355 A RU 2013154355A RU 2013154355/15 A RU2013154355/15 A RU 2013154355/15A RU 2013154355 A RU2013154355 A RU 2013154355A RU 2013154355 A RU2013154355 A RU 2013154355A
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gdc
patient
mesothelioma
effective amount
therapeutically effective
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Мика К. Деринк
ЛОШЛЬ Дженнифер О`ХАРА
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Ф. Хоффманн-Ля Рош Аг
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
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    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
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Abstract

1. GDC-0980, имеющий структуру:для применения для лечения мезотелиомы.2. Применение GDC-0980, имеющего структуру:для получения лекарственного средства для лечения мезотелиомы.3. Применение GDC-0980, имеющего структуру:для лечения мезотелиомы.4. Способ лечения мезотелиомы, включающий введение пациенту с мезотелиомой терапевтически эффективного количества GDC-0980, имеющего структуру:5. Способ по п. 4, когда пациент имеет злокачественную плевральную мезотелиому.6. Способ по п. 4, когда пациента ранее лечили химиотерапией, лучевой терапией и/или хирургической резекцией.7. Способ по п. 6, когда пациента ранее лечили одним или более чем одним химиотерапевтическим агентом, выбранным из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба и сорафениба.8. Способ по п. 4, в котором GDC-0980 вводится пациенту ежесуточно с интервалами три недели или четыре недели.9. Способ по п. 8, в котором после трехнедельного интервала следует однонедельный перерыв, когда пациенту не вводится GDC-0980.10. Способ по п. 4, в котором GDC-0980 вводится перорально.11. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 1 мг до 100 мг в сутки на массу тела пациента.12. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 10 мг до 50 мг в сутки в зависимости от массы тела пациента.13. Способ по п. 4, кроме того, включающий введение химиотерапевтического агента, выбранного из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба или сорафениба.14. Способ по п. 4, в котором GDC-0980 приготовлен в виде композиции с ингредиентом,

Claims (15)

1. GDC-0980, имеющий структуру:
Figure 00000001
для применения для лечения мезотелиомы.
2. Применение GDC-0980, имеющего структуру:
Figure 00000002
для получения лекарственного средства для лечения мезотелиомы.
3. Применение GDC-0980, имеющего структуру:
Figure 00000003
для лечения мезотелиомы.
4. Способ лечения мезотелиомы, включающий введение пациенту с мезотелиомой терапевтически эффективного количества GDC-0980, имеющего структуру:
Figure 00000004
5. Способ по п. 4, когда пациент имеет злокачественную плевральную мезотелиому.
6. Способ по п. 4, когда пациента ранее лечили химиотерапией, лучевой терапией и/или хирургической резекцией.
7. Способ по п. 6, когда пациента ранее лечили одним или более чем одним химиотерапевтическим агентом, выбранным из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба и сорафениба.
8. Способ по п. 4, в котором GDC-0980 вводится пациенту ежесуточно с интервалами три недели или четыре недели.
9. Способ по п. 8, в котором после трехнедельного интервала следует однонедельный перерыв, когда пациенту не вводится GDC-0980.
10. Способ по п. 4, в котором GDC-0980 вводится перорально.
11. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 1 мг до 100 мг в сутки на массу тела пациента.
12. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 10 мг до 50 мг в сутки в зависимости от массы тела пациента.
13. Способ по п. 4, кроме того, включающий введение химиотерапевтического агента, выбранного из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба или сорафениба.
14. Способ по п. 4, в котором GDC-0980 приготовлен в виде композиции с ингредиентом, выбранным из микрокристаллической целлюлозы, моногидрата лактозы, кроскармеллозы натрия, коповидона и стеарата магния.
15. Способ по п. 4, в котором GDC-0980 приготовлен в виде композиции с фармацевтически приемлемым скользящим веществом, выбранным из диоксида кремния, порошковой целлюлозы, микрокристаллической целлюлозы, стеаратов металлов, алюмосиликата натрия, бензоата натрия, карбоната кальция, силиката кальция, кукурузного крахмала, карбоната магния, талька, не содержащего асбест, стеаровета С, крахмала, крахмала 1500, лаурилсульфата магния, оксида магния и их комбинаций.
RU2013154355/15A 2011-06-03 2012-06-01 Способ лечения мезотелиомы ингибитором рi3к RU2013154355A (ru)

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US201161492966P 2011-06-03 2011-06-03
US61/492,966 2011-06-03
PCT/EP2012/060341 WO2012164060A1 (en) 2011-06-03 2012-06-01 Methods of treating mesothelioma with a pi3k inhibitor compound

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MX2013006858A (es) 2010-12-16 2013-07-29 Hoffmann La Roche Compuesto triciclicos inhibidores de la pi3k y metodos de uso.
CA2883513A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag Process for making thienopyrimidine compounds
CN105307669A (zh) * 2013-05-23 2016-02-03 戊瑞治疗有限公司 治疗癌症的方法
HK1223286A1 (zh) 2013-05-29 2017-07-28 西格诺药品有限公司 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法
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JP6592097B2 (ja) * 2014-10-30 2019-10-16 ビッグ ディーエヌエイ リミテッドBig Dna Ltd 併用療法
SI3316867T1 (sl) * 2015-06-30 2021-08-31 Genentech, Inc. Tablete s takojšnjim sproščanjem, ki vsebujejo zdravilo in postopek za pripravo tablet
WO2018234584A1 (en) 2017-06-23 2018-12-27 Almirall, S.A. Pharmaceutical compositions comprising dimethyl fumarate
US11103594B2 (en) 2018-02-01 2021-08-31 Imam Abdulrahman Bin Faisal University Hierarchical siliceous mesosilicalite nanocarrier loaded with platinum(II) complex

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SI1934174T1 (sl) 2005-10-07 2011-08-31 Exelixis Inc Inhibitorji MEK in postopki za njihovo uporabo
KR101101443B1 (ko) * 2006-08-14 2012-01-03 시코르, 인크. 페메트렉세드의 중간체의 제조 방법
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US20120308562A1 (en) 2012-12-06
AR086647A1 (es) 2014-01-15
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