RU2014126396A - Гидрохлорид производного пуринона - Google Patents
Гидрохлорид производного пуринона Download PDFInfo
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- RU2014126396A RU2014126396A RU2014126396A RU2014126396A RU2014126396A RU 2014126396 A RU2014126396 A RU 2014126396A RU 2014126396 A RU2014126396 A RU 2014126396A RU 2014126396 A RU2014126396 A RU 2014126396A RU 2014126396 A RU2014126396 A RU 2014126396A
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- -1 Purinone Derivative Hydrochloride Chemical class 0.000 title claims 3
- 239000013078 crystal Substances 0.000 claims abstract 14
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 9
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 8
- UQYDCIJFACDXSG-GMUIIQOCSA-N 6-amino-9-[(3r)-1-but-2-ynoylpyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one;hydrochloride Chemical compound Cl.C1N(C(=O)C#CC)CC[C@H]1N1C(=O)N(C=2C=CC(OC=3C=CC=CC=3)=CC=2)C2=C(N)N=CN=C21 UQYDCIJFACDXSG-GMUIIQOCSA-N 0.000 claims abstract 5
- 238000000113 differential scanning calorimetry Methods 0.000 claims abstract 4
- 201000010099 disease Diseases 0.000 claims abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 4
- 208000023275 Autoimmune disease Diseases 0.000 claims abstract 2
- 208000026935 allergic disease Diseases 0.000 claims abstract 2
- 208000027866 inflammatory disease Diseases 0.000 claims abstract 2
- 230000002265 prevention Effects 0.000 claims abstract 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229940124291 BTK inhibitor Drugs 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 208000001435 Thromboembolism Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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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
- A61K31/495—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
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
1. Гидрохлорид 6-амино-9-[(3R)-1-(2-бутиноил)-3-пирролидинил]-7-(4-фенокси-фенил)-7,9-дигидро-8H-пурин-8-она.2. Кристаллы гидрохлорида 6-амино-9-[(3R)-1-(2-бутиноил)-3-пирролидинил]-7-(4-феноксифенил)-7,9-дигидро-8H-пурин-8-она.3. Кристаллы по п. 2, имеющие на порошковой дифракционной рентгенограмме по меньшей мере 2 или больше пиков при углах 2θ, выбранных из примерно 8,11, 8,43, 11,57, 12,73, 13,85, 14,20, 14,67, 14,91, 15,94, 16,64, 18,06, 19,74, 20,42, 21,05, 22,57, 23,21, 23,85 и 24,70 градусов.4. Кристаллы по п. 2 или 3, имеющие на порошковой дифракционной рентгенограмме пики при углах 2θ, выбранных из примерно 8,11, 8,43, 14,20, 14,67, 14,91 и 23,21 градусов.5. Кристаллы по п. 2 или 3, имеющие на порошковой дифракционной рентгенограмме пики при углах 2θ, выбранных из примерно 8,11, 8,43, 11,57, 12,73, 13,85, 14,20, 14,67, 14,91, 15,94, 16,64, 18,06, 19,74, 20,42, 21,05, 22,57, 23,21, 23,85 и 24,70 градусов.6. Кристаллы по п. 2 или 3, характеризующиеся порошковой дифракционной рентгенограммой, приведенной на фиг. 3.7. Кристаллы по п. 2, имеющие эндотермический пик при температуре пика 216°C при исследовании методом дифференциальной сканирующей калориметрии.8. Кристаллы по п. 2 или 7, характеризующиеся графиком дифференциальной сканирующей калориметрии, приведенным на фиг. 4.9. Фармацевтическая композиция, содержащая гидрохлорид 6-амино-9-[(3R)-1-(2-бутиноил)-3-пирролидинил]-7-(4-феноксифенил)-7,9-дигидро-8H-пурин-8-она.10. Фармацевтическая композиция по п. 9, которая является ингибитором Btk.11. Фармацевтическая композиция по п. 10, которая является средством для профилактики и/или лечения связанных с Btk заболеваний.12. Фармацевтическая композиция по п. 11, причем связанное с Btk заболевание является аллергическим заболеванием, аутоиммунным заболеванием, воспалительным заболеванием, тромбоэмболич
Claims (13)
1. Гидрохлорид 6-амино-9-[(3R)-1-(2-бутиноил)-3-пирролидинил]-7-(4-фенокси-фенил)-7,9-дигидро-8H-пурин-8-она.
2. Кристаллы гидрохлорида 6-амино-9-[(3R)-1-(2-бутиноил)-3-пирролидинил]-7-(4-феноксифенил)-7,9-дигидро-8H-пурин-8-она.
3. Кристаллы по п. 2, имеющие на порошковой дифракционной рентгенограмме по меньшей мере 2 или больше пиков при углах 2θ, выбранных из примерно 8,11, 8,43, 11,57, 12,73, 13,85, 14,20, 14,67, 14,91, 15,94, 16,64, 18,06, 19,74, 20,42, 21,05, 22,57, 23,21, 23,85 и 24,70 градусов.
4. Кристаллы по п. 2 или 3, имеющие на порошковой дифракционной рентгенограмме пики при углах 2θ, выбранных из примерно 8,11, 8,43, 14,20, 14,67, 14,91 и 23,21 градусов.
5. Кристаллы по п. 2 или 3, имеющие на порошковой дифракционной рентгенограмме пики при углах 2θ, выбранных из примерно 8,11, 8,43, 11,57, 12,73, 13,85, 14,20, 14,67, 14,91, 15,94, 16,64, 18,06, 19,74, 20,42, 21,05, 22,57, 23,21, 23,85 и 24,70 градусов.
6. Кристаллы по п. 2 или 3, характеризующиеся порошковой дифракционной рентгенограммой, приведенной на фиг. 3.
7. Кристаллы по п. 2, имеющие эндотермический пик при температуре пика 216°C при исследовании методом дифференциальной сканирующей калориметрии.
8. Кристаллы по п. 2 или 7, характеризующиеся графиком дифференциальной сканирующей калориметрии, приведенным на фиг. 4.
9. Фармацевтическая композиция, содержащая гидрохлорид 6-амино-9-[(3R)-1-(2-бутиноил)-3-пирролидинил]-7-(4-феноксифенил)-7,9-дигидро-8H-пурин-8-она.
10. Фармацевтическая композиция по п. 9, которая является ингибитором Btk.
11. Фармацевтическая композиция по п. 10, которая является средством для профилактики и/или лечения связанных с Btk заболеваний.
12. Фармацевтическая композиция по п. 11, причем связанное с Btk заболевание является аллергическим заболеванием, аутоиммунным заболеванием, воспалительным заболеванием, тромбоэмболическим заболеванием, костным заболеванием или злокачественным новообразованием.
13. Фармацевтическая композиция по п. 12, причем злокачественное новообразование является неходжкинской лимфомой.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2011-259662 | 2011-11-29 | ||
JP2011259662 | 2011-11-29 | ||
PCT/JP2012/080769 WO2013081016A1 (ja) | 2011-11-29 | 2012-11-28 | プリノン誘導体塩酸塩 |
Related Child Applications (1)
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RU2017111078A Division RU2750538C2 (ru) | 2011-11-29 | 2012-11-28 | Гидрохлорид производного пуринона |
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RU2014126396A true RU2014126396A (ru) | 2016-01-27 |
RU2615999C2 RU2615999C2 (ru) | 2017-04-12 |
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RU2017111078A RU2750538C2 (ru) | 2011-11-29 | 2012-11-28 | Гидрохлорид производного пуринона |
RU2014126396A RU2615999C2 (ru) | 2011-11-29 | 2012-11-28 | Гидрохлорид производного пуринона |
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Country | Link |
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US (8) | US9199997B2 (ru) |
EP (1) | EP2786996B1 (ru) |
JP (1) | JP5704252B2 (ru) |
KR (3) | KR20180034705A (ru) |
CN (1) | CN103958513B (ru) |
AU (2) | AU2012344839B2 (ru) |
BR (2) | BR112014012727B1 (ru) |
CA (1) | CA2857150C (ru) |
CY (1) | CY1118376T1 (ru) |
DK (1) | DK2786996T3 (ru) |
ES (1) | ES2601219T3 (ru) |
HK (1) | HK1197819A1 (ru) |
HR (1) | HRP20161377T1 (ru) |
HU (1) | HUE031094T2 (ru) |
IL (1) | IL232822B (ru) |
LT (1) | LT2786996T (ru) |
MX (1) | MX353548B (ru) |
MY (1) | MY170062A (ru) |
NZ (1) | NZ626750A (ru) |
PH (1) | PH12014501503A1 (ru) |
PL (1) | PL2786996T3 (ru) |
PT (1) | PT2786996T (ru) |
RS (1) | RS55542B1 (ru) |
RU (2) | RU2750538C2 (ru) |
SG (1) | SG11201402658YA (ru) |
SI (1) | SI2786996T1 (ru) |
SM (1) | SMT201600426B (ru) |
TW (1) | TW201329078A (ru) |
WO (1) | WO2013081016A1 (ru) |
ZA (1) | ZA201404792B (ru) |
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