RU2016144187A - Твердые формы фармацевтически активного соединения - Google Patents

Твердые формы фармацевтически активного соединения Download PDF

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RU2016144187A
RU2016144187A RU2016144187A RU2016144187A RU2016144187A RU 2016144187 A RU2016144187 A RU 2016144187A RU 2016144187 A RU2016144187 A RU 2016144187A RU 2016144187 A RU2016144187 A RU 2016144187A RU 2016144187 A RU2016144187 A RU 2016144187A
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solid form
form according
theta
values
compound
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RU2016144187A
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RU2016144187A3 (ru
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Рудольф БЕНЦ
Ральф ДИОДОНЕ
Чжунцзян Цзя
Бхарат ПАТЕЛЬ
Урс ШВИТТЕР
Дюк Сун ЧОЙ
Нинсинь ЯНЬ
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Ф. Хоффманн-Ля Рош Аг
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (18)

1. Твердая форма соединения (1)
Figure 00000001
выбранная из:
a) по существу аморфной формы соединения (1);
b) полугидрата, гидрата, полусольвата или сольвата соединения (1); или
c) полиморфа соединения (1); или
d) фармацевтически приемлемой соли соединения (1).
2. Твердая форма по п. 1, отличающаяся тем, что она представляет собой полиморф, гидрат, полугидрат, сольват, полусольват или фармацевтически приемлемую соль.
3. Твердая форма по п. 1, отличающаяся тем, что она представляет собой аморфную форму.
4. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД (рентгеновская порошковая дифракция) со значениями 2 тета 4,9, 6,9, 7,7, 9,1, 10,9, 13,5, 14,5, 17,2, 20,4, 22,3 и 25,5.
5. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД со значениями 2 тета 4,1, 5,0, 5,7, 6,3, 6,9, 7,9, 8,1, 9,0, 10,0, 14,3 и 19,5.
6. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД со значениями 2 тета 5,9, 8,3, 9,5, 10,1, 11,3, 14,2, 15,8, 17,6, 19,0, 19,4, 19,8, 20,3 и 25,5.
7. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД со значениями 2 тета 5,1, 8,0, 8,3, 8,8, 9,3, 10,0, 10,3, 13,7, 14,3, 18,7, 20,2, 20,8 и 27,6.
8. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД со значениями 2 тета 3,9, 7,8, 8,7, 9,1, 13,7, 14,5, 18,2 и 20,3.
9. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД со значениями 2 тета 5,5, 7,4, 14,5, 14,8, 15,6, 16,9, 17,8, 18,6, 19,9, 20,5, 24,8 и 26,7.
10. Твердая форма по п. 1 или 2, характеризуемая дифрактограммой РПД со значениями 2 тета 6,6, 10,7, 14,6, 15,7, 16,0, 16,4, 18,9, 19,8, 21,4, 22,0, 25,3 и 26,1.
11. Твердая форма по п. 3, характеризуемая волновыми числами в спектре ИК-Фурье (инфракрасная спектроскопия на основе преобразования Фурье), см-1: 1705, 1687, 1600, 1587, 1525, 1483, 1409, 1367, 1343, 1299, 1276, 1250, 1230, 1221, 1178, 1128, 1086, 1034, 902, 885, 817, 778, 765 и 729.
12. Фармацевтическая композиция, содержащая одну или несколько твердых форм, охарактеризованных в любом из пп. 1-11, вместе с фармацевтически приемлемыми адъювантами или эксципиентами.
RU2016144187A 2014-04-15 2015-04-13 Твердые формы фармацевтически активного соединения RU2016144187A (ru)

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US201461979649P 2014-04-15 2014-04-15
US61/979,649 2014-04-15
PCT/EP2015/057937 WO2015158648A1 (en) 2014-04-15 2015-04-13 Solid forms of a pharmaceutically active compound

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CN (1) CN106458886A (ru)
AR (1) AR100095A1 (ru)
AU (1) AU2015249018A1 (ru)
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IL (1) IL247974A0 (ru)
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PL3458101T3 (pl) 2016-05-20 2021-05-31 F. Hoffmann-La Roche Ag Koniugaty PROTAC-przeciwciało i sposoby ich stosowania
WO2019213106A1 (en) 2018-04-30 2019-11-07 Teva Pharmaceuticals International Gmbh Solid state forms of idasanutlin
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

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US8354444B2 (en) * 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
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US20130245089A1 (en) * 2012-03-19 2013-09-19 Hoffmann-La Roche Inc. Method for administration
US9216170B2 (en) * 2012-03-19 2015-12-22 Hoffmann-La Roche Inc. Combination therapy for proliferative disorders
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JP6887980B2 (ja) 2021-06-16
RU2016144187A3 (ru) 2018-11-13
MA39877A (fr) 2017-02-22
AU2015249018A1 (en) 2016-10-06
JP2019055960A (ja) 2019-04-11
CA2943571A1 (en) 2015-10-22
EP3131878A1 (en) 2017-02-22
US20170037005A1 (en) 2017-02-09
EP3459933B1 (en) 2022-08-24
AR100095A1 (es) 2016-09-07
WO2015158648A1 (en) 2015-10-22
EP3459933A2 (en) 2019-03-27
EP3459933A3 (en) 2019-05-29
MX2016013439A (es) 2016-11-17
KR20160138307A (ko) 2016-12-02
JP2017511362A (ja) 2017-04-20
PL3459933T3 (pl) 2023-01-23
ZA201606653B (en) 2018-05-30
IL247974A0 (en) 2016-11-30
BR112016023767A2 (pt) 2017-08-15
US10227298B2 (en) 2019-03-12

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