RU2013109393A - Безилатная соль ингибитора втк - Google Patents
Безилатная соль ингибитора втк Download PDFInfo
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- RU2013109393A RU2013109393A RU2013109393/04A RU2013109393A RU2013109393A RU 2013109393 A RU2013109393 A RU 2013109393A RU 2013109393/04 A RU2013109393/04 A RU 2013109393/04A RU 2013109393 A RU2013109393 A RU 2013109393A RU 2013109393 A RU2013109393 A RU 2013109393A
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- 229940124291 BTK inhibitor Drugs 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 41
- 239000007787 solid Substances 0.000 claims abstract 27
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 18
- 229940125782 compound 2 Drugs 0.000 claims abstract 3
- 239000012535 impurity Substances 0.000 claims abstract 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 0 COCCOc(cc1)ccc1Nc1nc(Nc2cccc(NC(C=C)=O)c2)c(*)cn1 Chemical compound COCCOc(cc1)ccc1Nc1nc(Nc2cccc(NC(C=C)=O)c2)c(*)cn1 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N OS(c1ccccc1)(=O)=O Chemical compound OS(c1ccccc1)(=O)=O SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P37/02—Immunomodulators
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- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
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Abstract
1. Соединение 2:2. Соединение по п.1, отличающееся тем, что указанное соединение находится в твердой форме.3. Соединение по п.2, отличающееся тем, что указанное соединение является кристаллическим.4. Соединение по п.3, отличающееся тем, что указанное соединение представляет собой кристаллическое твердое вещество, по существу, не содержащее аморфного соединения 2.5. Соединение по п.1, отличающееся тем, что указанное соединение, по существу, не содержит примесей.6. Соединение по п.2, отличающееся тем, что указанная твердая форма представляет собой Форму Р1.7. Соединение по п.6, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме одного или более пиков, выбранных из пиков при примерно 6,21, примерно 9,48 и примерно 13,29 градусов 2-θ.8. Соединение по п.7, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме по меньшей мере двух пиков, выбранных из пиков при примерно 6,21, примерно 9,48 и примерно 13,29 градусов 2-θ.9. Соединение по п.6, отличающееся тем, что указанная твердая форма характеризуется порошковой рентгеновской дифрактограммой, по существу, аналогичной приведенной на Фигуре 2.10. Соединение по п.2, отличающееся тем, что указанная твердая форма представляет собой Форму Р22.11. Соединение по п.10, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме одного или более пиков, выбранных из пиков при примерно 7,29, примерно 8,38 и примерно 11,12 градусов 2-θ.12. Соединение по п.11, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентг�
Claims (22)
1. Соединение 2:
2. Соединение по п.1, отличающееся тем, что указанное соединение находится в твердой форме.
3. Соединение по п.2, отличающееся тем, что указанное соединение является кристаллическим.
4. Соединение по п.3, отличающееся тем, что указанное соединение представляет собой кристаллическое твердое вещество, по существу, не содержащее аморфного соединения 2.
5. Соединение по п.1, отличающееся тем, что указанное соединение, по существу, не содержит примесей.
6. Соединение по п.2, отличающееся тем, что указанная твердая форма представляет собой Форму Р1.
7. Соединение по п.6, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме одного или более пиков, выбранных из пиков при примерно 6,21, примерно 9,48 и примерно 13,29 градусов 2-θ.
8. Соединение по п.7, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме по меньшей мере двух пиков, выбранных из пиков при примерно 6,21, примерно 9,48 и примерно 13,29 градусов 2-θ.
9. Соединение по п.6, отличающееся тем, что указанная твердая форма характеризуется порошковой рентгеновской дифрактограммой, по существу, аналогичной приведенной на Фигуре 2.
10. Соединение по п.2, отличающееся тем, что указанная твердая форма представляет собой Форму Р22.
11. Соединение по п.10, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме одного или более пиков, выбранных из пиков при примерно 7,29, примерно 8,38 и примерно 11,12 градусов 2-θ.
12. Соединение по п.11, отличающееся тем, что указанная твердая форма характеризуется наличием на порошковой рентгеновской дифрактограмме по меньшей мере двух пиков, выбранных из пиков при примерно 7,29, примерно 8,38 и примерно 11,12 градусов 2-θ.
13. Соединение по п.10, отличающееся тем, что указанная твердая форма характеризуется порошковой рентгеновской дифрактограммой, по существу, аналогичной приведенной на фигуре 6.
14. Композиция, содержащая соединение по п.1 и фармацевтически приемлемый носитель или вспомогательное вещество.
15. Соединение по п.2, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере одним пиком, выбранным из пиков на порошковой рентгеновской дифрактограмме Формы Р1, приведенной на фигуре 2.
16. Соединение по п.15, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере двумя пиками, выбранными из пиков на порошковой рентгеновской дифрактограмме формы Р1, приведенной на фигуре 2.
17. Соединение по п.16, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере тремя пиками, выбранными из пиков на порошковой рентгеновской дифрактограмме формы Р1, приведенной на фигуре 2.
18. Соединение по п.17, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере четырьмя пиками, выбранными из пиков на порошковой рентгеновской дифрактограмме формы Р1, приведенной на фигуре 2.
19. Соединение по п.2, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере одним пиком, выбранным из пиков на порошковой рентгеновской дифрактограмме формы Р22, приведенной на фигуре 6.
20. Соединение по п.19, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере двумя пиками, выбранными из пиков на порошковой рентгеновской дифрактограмме формы Р22, приведенной на фигуре 6.
21. Соединение по п.20, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере тремя пиками, выбранными из пиков на порошковой рентгеновской дифрактограмме формы Р22, приведенной на фигуре 6.
22. Соединение по п.21, отличающееся тем, что указанная твердая форма характеризуется по меньшей мере четырьмя пиками, выбранными из пиков на порошковой рентгеновской дифрактограмме формы Р22, приведенной на фигуре 6.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37234910P | 2010-08-10 | 2010-08-10 | |
| US61/372,349 | 2010-08-10 | ||
| PCT/US2011/046926 WO2012021444A1 (en) | 2010-08-10 | 2011-08-08 | Besylate salt of a btk inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2013109393A true RU2013109393A (ru) | 2014-09-20 |
Family
ID=45567913
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013109393/04A RU2013109393A (ru) | 2010-08-10 | 2011-08-08 | Безилатная соль ингибитора втк |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8563568B2 (ru) |
| EP (2) | EP2603081B1 (ru) |
| JP (1) | JP6068340B2 (ru) |
| KR (1) | KR20130099040A (ru) |
| CN (2) | CN103096716B (ru) |
| AR (1) | AR082600A1 (ru) |
| AU (1) | AU2011289604C1 (ru) |
| BR (1) | BR112013003388A2 (ru) |
| CA (1) | CA2807051A1 (ru) |
| DK (1) | DK2603081T3 (ru) |
| ES (1) | ES2617763T3 (ru) |
| IL (1) | IL224271A (ru) |
| MX (1) | MX336875B (ru) |
| MY (1) | MY160734A (ru) |
| NZ (1) | NZ607845A (ru) |
| PH (1) | PH12013500246A1 (ru) |
| PT (1) | PT2603081T (ru) |
| RU (1) | RU2013109393A (ru) |
| SG (1) | SG187796A1 (ru) |
| TW (1) | TWI533872B (ru) |
| WO (1) | WO2012021444A1 (ru) |
| ZA (1) | ZA201301802B (ru) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2673077C2 (ru) * | 2012-03-15 | 2018-11-22 | Селджен Авиломикс Рисерч, Инк. | Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста |
| RU2711077C2 (ru) * | 2012-03-15 | 2020-01-15 | Селджен Кар Ллс | Соли ингибитора киназы рецептора эпидермального фактора роста |
Families Citing this family (92)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2585902T3 (es) | 2006-09-22 | 2016-10-10 | Pharmacyclics Llc | Inhibidores de tirosina cinasa de Bruton |
| US20120101114A1 (en) | 2007-03-28 | 2012-04-26 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| EA029131B1 (ru) | 2008-05-21 | 2018-02-28 | Ариад Фармасьютикалз, Инк. | Фосфорсодержащие производные в качестве ингибиторов киназы |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| DK2361248T3 (en) | 2008-06-27 | 2019-01-14 | Celgene Car Llc | Heteroberl compounds and uses thereof |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
| RU2012114902A (ru) | 2009-09-16 | 2013-10-27 | Авила Терапьютикс, Инк. | Конъюгаты и ингибиторы протеинкиназы |
| CN102812167A (zh) | 2009-12-30 | 2012-12-05 | 阿维拉制药公司 | 蛋白的配体-介导的共价修饰 |
| NZ702485A (en) | 2010-06-03 | 2016-04-29 | Pharmacyclics Llc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| KR20130099040A (ko) | 2010-08-10 | 2013-09-05 | 셀진 아빌로믹스 리서치, 인코포레이티드 | Ｂｔｋ 억제제의 베실레이트 염 |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| JP5957460B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | 複素環式化合物またはその使用 |
| JP5957003B2 (ja) | 2010-11-10 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | 変異体選択的ｅｇｆｒ阻害剤およびその使用 |
| CA2832504C (en) | 2011-05-04 | 2019-10-01 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| AR088570A1 (es) | 2011-10-28 | 2014-06-18 | Celgene Avilomics Res Inc | Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2673077C2 (ru) * | 2012-03-15 | 2018-11-22 | Селджен Авиломикс Рисерч, Инк. | Твёрдые формы ингибитора киназы рецептора эпидермального фактора роста |
| RU2711077C2 (ru) * | 2012-03-15 | 2020-01-15 | Селджен Кар Ллс | Соли ингибитора киназы рецептора эпидермального фактора роста |
| RU2711077C9 (ru) * | 2012-03-15 | 2020-08-11 | Селджен Кар Ллс | Соли ингибитора киназы рецептора эпидермального фактора роста |
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