CN101861314A - N4-[(2,2-二氟-4h-苯并[1,4]嗪-3-酮)-6-基]-5-氟-n2-[3-(甲基氨基羰基亚甲基氧基)苯基]-2,4-嘧啶二胺的1-羟基-2-萘甲酸盐 - Google Patents
N4-[(2,2-二氟-4h-苯并[1,4]嗪-3-酮)-6-基]-5-氟-n2-[3-(甲基氨基羰基亚甲基氧基)苯基]-2,4-嘧啶二胺的1-羟基-2-萘甲酸盐 Download PDFInfo
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Abstract
Description
角2θ(度) | 相对强度(%) | 角2θ(度) | 相对强度(%) |
8.0 | 68.7 | 22.4 | 16.5 |
8.9 | 36.5 | 23.0 | 24.1 |
11.6 | 42.6 | 23.2 | 19.9 |
13.2 | 42.5 | 23.5 | 22.8 |
13.5 | 23.8 | 23.6 | 20.9 |
角2θ(度) | 相对强度(%) | 角2θ(度) | 相对强度(%) |
14.0 | 18.7 | 24.1 | 38.1 |
15.3 | 15.0 | 24.5 | 100.0 |
15.6 | 17.4 | 24.7 | 20.6 |
16.1 | 44.5 | 26.6 | 41.1 |
16.4 | 20.1 | 27.5 | 12.3 |
17.3 | 14.5 | 27.7 | 73.7 |
17.5 | 21.4 | 28.1 | 14.1 |
17.8 | 30.3 | 29.3 | 16.6 |
19.0 | 28.9 | 29.5 | 11.4 |
19.8 | 54.0 | 31.2 | 11.8 |
20.0 | 28.8 | 32.4 | 14.4 |
20.4 | 13.0 | 33.4 | 22.5 |
22.1 | 15.0 |
角2θ(度) | 相对强度(%) | 角2θ(度) | 相对强度(%) |
8.0 | 72.5 | 18.9 | 11.7 |
8.9 | 41.3 | 19.0 | 13.2 |
9.4 | 10.5 | 19.9 | 15.8 |
11.4 | 11.5 | 20.1 | 25.1 |
11.6 | 43.0 | 23.0 | 15.2 |
13.5 | 16.6 | 23.2 | 11.5 |
14.0 | 19.2 | 23.5 | 10.2 |
15.3 | 13.3 | 23.6 | 12.1 |
15.7 | 10.2 | 24.1 | 28.5 |
16.0 | 14.3 | 24.4 | 14.1 |
16.1 | 17.6 | 24.5 | 100.0 |
16.4 | 17.1 | 24.7 | 11.9 |
17.5 | 19.4 | 27.7 | 58.5 |
17.9 | 20.3 |
波数(cm-1) | 波数(cm-1) | 波数(cm-1) | 波数(cm-1) |
3230*(w) | 1501(w) | 1174(m) | 810(w) |
3069(w) | 1455(m) | 1161(m) | 796(m) |
3015(w) | 1431(s) | 1152(m) | 764(s) |
1717(s) | 1407(s) | 1107(w) | 747(s) |
波数(cm-1) | 波数(cm-1) | 波数(cm-1) | 波数(cm-1) |
1669(m) | 1364(w) | 1078(s) | 734(w) |
1659(m) | 1331(w) | 1020(w) | 721(w) |
1625(m) | 1316(w) | 928(w) | 683(m) |
1608(m) | 1283(w) | 888(m) | 653(m) |
1587(m) | 1272(w) | 877(w) | |
1569(m) | 1228(m) | 858(s) | |
1523(m) | 1212(m) | 823(m) |
波数(cm-1) | 波数(cm-1) | 波数(cm-1) | 波数(cm-1) |
3092(w) | 1473(w) | 1253(m) | 332(w) |
3071(w) | 1465(w) | 1205(m) | 302(w) |
1679(w) | 1434(m) | 1162(w) | 286(w) |
1659(m) | 1414(w) | 1026(w) | 253(w) |
1626(m) | 1379(m) | 998(s) | 221(m) |
波数(cm-1) | 波数(cm-1) | 波数(cm-1) | 波数(cm-1) |
1611(w) | 1365(m) | 879(w) | 192(w) |
1596(w) | 1353(m) | 726(m) | 156(s) |
1584(w) | 1333(s) | 542(w) | 130(m) |
1574(w) | 1296(m) | 495(w) | 110(s) |
1525(m) | 1276(w) | 434(w) | 91(s) |
1502(m) | 1260(m) | 352(w) | 62(s) |
化学位移(ppm) | 强度 | 化学位移(ppm) | 强度 |
176.8 | 6.48 | 128.4 | 4.88 |
171.8 | 6.04 | 126.9 | 9.39 |
159.4 | 10.46 | 125.8 | 11.22 |
157.5 | 4.33 | 123.0 | 6.03 |
150.0 | 4.66 | 121.6 | 9.38 |
148.3 | 4.83 | 118.2 | 7.96 |
140.9 | 6.12 | 110.9 | 12 |
化学位移(ppm) | 强度 | 化学位移(ppm) | 强度 |
139.2 | 2.37 | 109.0 | 4.37 |
137.1 | 9.88 | 104.9 | 3.99 |
134.4 | 6.97 | 69.3 | 4.01 |
133.1 | 6.41 | 25.4 | 6.37 |
Claims (12)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US97003007P | 2007-09-05 | 2007-09-05 | |
US60/970,030 | 2007-09-05 | ||
PCT/IB2008/002288 WO2009031011A2 (en) | 2007-09-05 | 2008-08-27 | Xinafoate salt of n4-(2, 2-difluoro-4h-benz0 [1,4] 0xazin-3-one) -6-yl] -5-fluoro-n2- [3- (methylaminocar bonylmethyleneoxy) phenyl] 2, 4-pyrimidinediamine |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101861314A true CN101861314A (zh) | 2010-10-13 |
CN101861314B CN101861314B (zh) | 2013-07-24 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CN200880105757XA Expired - Fee Related CN101861314B (zh) | 2007-09-05 | 2008-08-27 | N4-[(2,2-二氟-4h-苯并[1,4]*嗪-3-酮)-6-基]-5-氟-n2-[3-(甲基氨基羰基亚甲基氧基)苯基]-2,4-嘧啶二胺的1-羟基-2-萘甲酸盐 |
Country Status (18)
Country | Link |
---|---|
US (3) | US8193181B2 (zh) |
EP (1) | EP2215087B1 (zh) |
JP (1) | JP2009084270A (zh) |
KR (2) | KR20120120453A (zh) |
CN (1) | CN101861314B (zh) |
AR (1) | AR068369A1 (zh) |
AU (1) | AU2008294473B2 (zh) |
BR (1) | BRPI0816278A2 (zh) |
CA (1) | CA2697495C (zh) |
ES (1) | ES2452965T3 (zh) |
HK (1) | HK1144685A1 (zh) |
IL (1) | IL203973A (zh) |
MX (1) | MX2010002518A (zh) |
NZ (1) | NZ583582A (zh) |
RU (1) | RU2458925C2 (zh) |
TW (1) | TWI371277B (zh) |
WO (1) | WO2009031011A2 (zh) |
ZA (1) | ZA201002356B (zh) |
Families Citing this family (29)
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GB0908772D0 (en) * | 2009-05-21 | 2009-07-01 | Astrazeneca Ab | New salts 756 |
SG175796A1 (en) | 2009-05-21 | 2011-12-29 | Astrazeneca Ab | Novel pyrimidine derivatives and their use in the treatment of cancer and further diseases |
WO2012154520A1 (en) | 2011-05-10 | 2012-11-15 | Merck Sharp & Dohme Corp. | Pyridyl aminopyridines as syk inhibitors |
WO2012154518A1 (en) | 2011-05-10 | 2012-11-15 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as syk inhibitors |
JP2014513686A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Syk阻害薬としてのアミノピリミジン |
US9216173B2 (en) | 2011-10-05 | 2015-12-22 | Merck Sharp & Dohme Corp. | 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors |
US8987456B2 (en) | 2011-10-05 | 2015-03-24 | Merck Sharp & Dohme Corp. | 3-pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors |
EP2763974B1 (en) | 2011-10-05 | 2016-09-14 | Merck Sharp & Dohme Corp. | Phenyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors |
US20130102596A1 (en) * | 2011-10-21 | 2013-04-25 | Rigel Pharmaceuticals, Inc. | Method and device for administering xinafoate salt of n4-(2,2-difluoro-4h-benzo [1,4]oxazin-3-one)-6-yl]-5-fluoro-n2-[3- (methylaminocarbonylmethyleneoxy) phenyl]2,4-pyrimidinediamine |
EP2863913B1 (en) | 2012-06-20 | 2018-09-12 | Merck Sharp & Dohme Corp. | Imidazolyl analogs as syk inhibitors |
EP2863914B1 (en) | 2012-06-20 | 2018-10-03 | Merck Sharp & Dohme Corp. | Pyrazolyl derivatives as syk inhibitors |
WO2013192088A1 (en) | 2012-06-22 | 2013-12-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
WO2013192098A1 (en) | 2012-06-22 | 2013-12-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
EP2884982B1 (en) | 2012-08-20 | 2017-09-20 | Merck Sharp & Dohme Corp. | SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
US9586931B2 (en) | 2012-09-28 | 2017-03-07 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as Syk inhibitors |
EP2931281B1 (en) | 2012-12-12 | 2018-01-17 | Merck Sharp & Dohme Corp. | Amino-pyrimidine-containing spleen tyrosine kinase inhibitors |
WO2014100314A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors |
US20140274873A1 (en) * | 2013-03-14 | 2014-09-18 | Allergan, Inc. | Composition of a sustained-release delivery and method of stabilizing proteins during fabrication process |
EP2988744A4 (en) | 2013-04-26 | 2016-11-02 | Merck Sharp & Dohme | THIAZOLE SUBSTITUTED AMINOHETEROARYL COMPOUNDS TYLOSINE KINASE SPLENIC INHIBITORS |
WO2014176216A1 (en) | 2013-04-26 | 2014-10-30 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors |
US9670196B2 (en) | 2013-12-20 | 2017-06-06 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors |
WO2015095445A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
WO2015094997A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
WO2015138273A1 (en) | 2014-03-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
WO2018189566A1 (en) * | 2017-04-10 | 2018-10-18 | Dorian Bevec | Use of a chemical compound as a therapeutic agent |
MX2021000611A (es) | 2018-07-18 | 2021-04-13 | Astrazeneca Ab | Una sal de xinafoato de un compuesto inhibidor de jak. |
EP3942045A1 (en) | 2019-03-21 | 2022-01-26 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
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US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
GB9808802D0 (en) * | 1998-04-24 | 1998-06-24 | Glaxo Group Ltd | Pharmaceutical formulations |
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
GB0208609D0 (en) * | 2002-04-13 | 2002-05-22 | Glaxo Group Ltd | Compositions |
JP2006506360A (ja) * | 2002-10-04 | 2006-02-23 | ファルマシア・コーポレーション | パーキンソン病の治療のための医薬組成物 |
KR20120062863A (ko) * | 2003-07-30 | 2012-06-14 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물 |
JP5315048B2 (ja) * | 2005-06-15 | 2013-10-16 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規チオトロピウム塩の製造方法、新規チオトロピウム塩及びその医薬組成物 |
KR101402398B1 (ko) * | 2006-06-30 | 2014-06-03 | 노파르티스 아게 | 퀴놀리논 유도체 및 이의 제약 조성물 |
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2008
- 2008-08-27 KR KR1020127024371A patent/KR20120120453A/ko not_active Application Discontinuation
- 2008-08-27 CN CN200880105757XA patent/CN101861314B/zh not_active Expired - Fee Related
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AU2008294473A1 (en) | 2009-03-12 |
AU2008294473B2 (en) | 2013-12-05 |
TW200927125A (en) | 2009-07-01 |
MX2010002518A (es) | 2010-03-26 |
JP2009084270A (ja) | 2009-04-23 |
TWI371277B (en) | 2012-09-01 |
US20100204232A1 (en) | 2010-08-12 |
US8486935B2 (en) | 2013-07-16 |
CA2697495A1 (en) | 2009-03-12 |
CA2697495C (en) | 2013-02-05 |
RU2458925C2 (ru) | 2012-08-20 |
RU2010108162A (ru) | 2011-09-10 |
AR068369A1 (es) | 2009-11-11 |
WO2009031011A3 (en) | 2009-04-30 |
HK1144685A1 (zh) | 2011-03-04 |
CN101861314B (zh) | 2013-07-24 |
EP2215087A2 (en) | 2010-08-11 |
BRPI0816278A2 (pt) | 2015-09-22 |
ZA201002356B (en) | 2010-12-29 |
KR101225233B1 (ko) | 2013-01-22 |
WO2009031011A2 (en) | 2009-03-12 |
ES2452965T3 (es) | 2014-04-03 |
IL203973A (en) | 2013-10-31 |
KR20120120453A (ko) | 2012-11-01 |
KR20100049688A (ko) | 2010-05-12 |
NZ583582A (en) | 2012-02-24 |
EP2215087B1 (en) | 2013-12-18 |
US8193181B2 (en) | 2012-06-05 |
US20120316160A1 (en) | 2012-12-13 |
US20130281446A1 (en) | 2013-10-24 |
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