JP2013511475A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013511475A5 JP2013511475A5 JP2012539175A JP2012539175A JP2013511475A5 JP 2013511475 A5 JP2013511475 A5 JP 2013511475A5 JP 2012539175 A JP2012539175 A JP 2012539175A JP 2012539175 A JP2012539175 A JP 2012539175A JP 2013511475 A5 JP2013511475 A5 JP 2013511475A5
- Authority
- JP
- Japan
- Prior art keywords
- ethyl
- oxy
- dimethylamino
- phenyl
- amino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 238000000034 method Methods 0.000 claims 32
- -1 2- (dimethylamino) ethyl Chemical group 0.000 claims 31
- 239000003814 drug Substances 0.000 claims 24
- 229940124597 therapeutic agent Drugs 0.000 claims 24
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 16
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 13
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical group CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 12
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 12
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 12
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 9
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 9
- 239000002904 solvent Substances 0.000 claims 9
- TTZSNFLLYPYKIL-UHFFFAOYSA-N n-[2-(dimethylamino)ethyl]-1-[3-[[4-[(2-methyl-1h-indol-5-yl)oxy]pyrimidin-2-yl]amino]phenyl]methanesulfonamide Chemical compound CN(C)CCNS(=O)(=O)CC1=CC=CC(NC=2N=C(OC=3C=C4C=C(C)NC4=CC=3)C=CN=2)=C1 TTZSNFLLYPYKIL-UHFFFAOYSA-N 0.000 claims 8
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 6
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 6
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 230000033115 angiogenesis Effects 0.000 claims 6
- 239000000010 aprotic solvent Substances 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 238000001816 cooling Methods 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 238000004090 dissolution Methods 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 238000010992 reflux Methods 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- SMRKYYXMQGTANS-UHFFFAOYSA-N N,N-dimethyl-N'-[4-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-2-yl]-N'-(3-methylphenyl)ethane-1,2-diamine Chemical compound CN(C)CCN(c1cccc(C)c1)c1nccc(Oc2ccc3[nH]c(C)cc3c2)n1 SMRKYYXMQGTANS-UHFFFAOYSA-N 0.000 claims 4
- 230000005764 inhibitory process Effects 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 239000003960 organic solvent Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 229940124530 sulfonamide Drugs 0.000 claims 4
- 150000003456 sulfonamides Chemical class 0.000 claims 4
- 206010064930 age-related macular degeneration Diseases 0.000 claims 3
- 150000001298 alcohols Chemical group 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 238000010438 heat treatment Methods 0.000 claims 3
- 208000002780 macular degeneration Diseases 0.000 claims 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- 239000008186 active pharmaceutical agent Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000009257 reactivity Effects 0.000 claims 2
- 230000004043 responsiveness Effects 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 1
- 125000004531 indol-5-yl group Chemical group [H]N1C([H])=C([H])C2=C([H])C(*)=C([H])C([H])=C12 0.000 claims 1
- 238000010899 nucleation Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000009331 sowing Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009101992592A CN102070618B (zh) | 2009-11-23 | 2009-11-23 | 一种化合物及其晶体 |
| CN200910199259.2 | 2009-11-23 | ||
| PCT/CN2010/078997 WO2011060746A1 (en) | 2009-11-23 | 2010-11-23 | Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013511475A JP2013511475A (ja) | 2013-04-04 |
| JP2013511475A5 true JP2013511475A5 (OSRAM) | 2014-01-16 |
| JP5758399B2 JP5758399B2 (ja) | 2015-08-05 |
Family
ID=44029398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012539175A Active JP5758399B2 (ja) | 2009-11-23 | 2010-11-23 | 化合物、その一定の新形態、その医薬組成物ならびに製剤化および使用の方法 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US8658658B2 (OSRAM) |
| EP (1) | EP2504331B1 (OSRAM) |
| JP (1) | JP5758399B2 (OSRAM) |
| KR (1) | KR101513784B1 (OSRAM) |
| CN (2) | CN102070618B (OSRAM) |
| AU (1) | AU2010321366B2 (OSRAM) |
| BR (1) | BR112012012138B1 (OSRAM) |
| CA (1) | CA2781066C (OSRAM) |
| DK (1) | DK2504331T3 (OSRAM) |
| ES (1) | ES2529105T3 (OSRAM) |
| IN (1) | IN2012DN04868A (OSRAM) |
| MX (1) | MX2012005926A (OSRAM) |
| MY (1) | MY161749A (OSRAM) |
| NZ (1) | NZ600266A (OSRAM) |
| PH (1) | PH12012500992A1 (OSRAM) |
| PL (1) | PL2504331T3 (OSRAM) |
| PT (1) | PT2504331E (OSRAM) |
| RU (1) | RU2507203C1 (OSRAM) |
| WO (1) | WO2011060746A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102070618B (zh) | 2009-11-23 | 2013-08-21 | 和记黄埔医药（上海）有限公司 | 一种化合物及其晶体 |
| BR122020023385B1 (pt) | 2014-06-19 | 2021-05-25 | Merial, Inc | composições parasiticidas compreendendo derivados de indol, métodos e usos dos mesmos |
| CN105985326B (zh) * | 2015-02-16 | 2020-04-14 | 上海宣创生物科技有限公司 | 嘧啶衍生物晶型ⅲ及其制备方法和用途 |
| WO2016187767A1 (en) * | 2015-05-25 | 2016-12-01 | Hutchison Medipharma Limited | Pharmaceutical compositions and use thereof |
| WO2018090324A1 (en) * | 2016-11-18 | 2018-05-24 | Hutchison Medipharma Limited | Method of treating solid tumors |
| JP2020164434A (ja) * | 2019-03-28 | 2020-10-08 | 上野製薬株式会社 | ２，６−ナフタレンビス（２−オキサゾリン）の製造方法 |
| CN115052605B (zh) * | 2020-03-09 | 2024-07-05 | 和记黄埔医药（上海）有限公司 | 抗pd-1抗体和多受体酪氨酸激酶抑制剂的药物组合及其使用方法 |
| US20240043409A1 (en) * | 2021-04-12 | 2024-02-08 | Mitoimmune Therapeutics Inc. | Crystalline forms of 5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-phenyl-n-(tetrahydro-2h-pyran-4-yl)-1h-indol-7-amine |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1976905A (zh) * | 2004-03-30 | 2007-06-06 | 大正制药株式会社 | 嘧啶衍生物以及与其应用有关的治疗方法 |
| WO2007035309A1 (en) | 2005-09-15 | 2007-03-29 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| DK2154967T5 (en) * | 2007-04-16 | 2014-11-17 | Hutchison Medipharma Entpr Ltd | Pyriminderivater |
| CN101289444B (zh) * | 2007-04-16 | 2012-01-04 | 和记黄埔医药（上海）有限公司 | 一种嘧啶衍生物及其医药用途 |
| TW201008933A (en) | 2008-08-29 | 2010-03-01 | Hutchison Medipharma Entpr Ltd | Pyrimidine compounds |
| CN102070618B (zh) * | 2009-11-23 | 2013-08-21 | 和记黄埔医药（上海）有限公司 | 一种化合物及其晶体 |
-
2009
- 2009-11-23 CN CN2009101992592A patent/CN102070618B/zh active Active
-
2010
- 2010-11-23 CA CA2781066A patent/CA2781066C/en active Active
- 2010-11-23 DK DK10831161.4T patent/DK2504331T3/en active
- 2010-11-23 JP JP2012539175A patent/JP5758399B2/ja active Active
- 2010-11-23 EP EP10831161.4A patent/EP2504331B1/en active Active
- 2010-11-23 AU AU2010321366A patent/AU2010321366B2/en active Active
- 2010-11-23 MY MYPI2012002250A patent/MY161749A/en unknown
- 2010-11-23 KR KR1020127015836A patent/KR101513784B1/ko active Active
- 2010-11-23 NZ NZ600266A patent/NZ600266A/en unknown
- 2010-11-23 ES ES10831161.4T patent/ES2529105T3/es active Active
- 2010-11-23 PT PT108311614T patent/PT2504331E/pt unknown
- 2010-11-23 PL PL10831161T patent/PL2504331T3/pl unknown
- 2010-11-23 CN CN201080052921.2A patent/CN102648194B/zh active Active
- 2010-11-23 IN IN4868DEN2012 patent/IN2012DN04868A/en unknown
- 2010-11-23 PH PH1/2012/500992A patent/PH12012500992A1/en unknown
- 2010-11-23 WO PCT/CN2010/078997 patent/WO2011060746A1/en not_active Ceased
- 2010-11-23 RU RU2012126112/04A patent/RU2507203C1/ru active
- 2010-11-23 US US13/510,249 patent/US8658658B2/en active Active
- 2010-11-23 MX MX2012005926A patent/MX2012005926A/es active IP Right Grant
- 2010-11-23 BR BR112012012138-3A patent/BR112012012138B1/pt active IP Right Grant
-
2013
- 2013-12-12 US US14/104,954 patent/US8946249B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013511475A5 (OSRAM) | ||
| JP4585610B2 (ja) | 治療用化合物のトシル酸塩およびその医薬組成物 | |
| JP6916969B1 (ja) | ３−（（１Ｒ，３Ｒ）−１−（２，６−ジフルオロ−４−（（１−（３−フルオロプロピル）アゼチジン−３−イル）アミノ）フェニル）−３−メチル−１，３，４，９−テトラヒドロ−２Ｈ−ピリド［３，４−ｂ］インドール−２−イル）−２，２−ジフルオロプロパン−１−オールの固体形態及び置換されたフェニル又はピリジニル部分を含む縮合三環式化合物を調製するための方法とそれらの使用方法 | |
| CN102453024B (zh) | 一种尼罗替尼盐酸盐晶型及其制备方法 | |
| JP6846574B2 (ja) | スルホンアミド化合物およびその使用 | |
| CN102827153B (zh) | 阿齐沙坦的晶型及其制备方法 | |
| TW200829584A (en) | Thiazole and oxazole-substituted arylamides | |
| CA2727378A1 (en) | New co-crystal compound of rivaroxaban and malonic acid | |
| RU2012126112A (ru) | Соединение, некоторые его новые формы, фармацевтические композиции на его основе и способы получения и применения | |
| CN109790123B (zh) | 新型衣壳蛋白装配抑制剂 | |
| JP2010539237A (ja) | Ｎ−（５−ｔｅｒｔ−ブチル−イソオキサゾール−３−イル）−Ｎ’−｛４−［７−（２−モルホリン−４−イル−エトキシ）イミダゾ［２，１−ｂ］［１，３］ベンゾチアゾール−２−イル］フェニル｝ウレアを含む固形、その組成物、及びその用途 | |
| CA3142444C (en) | CDK9 INHIBITOR POLYMORPH, POLYMORPH PREPARATION METHOD AND ASSOCIATED USES | |
| JP2013519665A (ja) | メシル酸イマチニブのα形の製造方法 | |
| CN105324375A (zh) | 盐酸尼洛替尼的多晶型形式 | |
| US12215083B2 (en) | Solid forms of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-n-benzylacetamide | |
| CN102807575B (zh) | 3-芳基-5-噻吩基-5H-噻唑并[3,2-a]嘧啶类衍生物及其应用 | |
| BR112020001775A2 (pt) | composto e processo para a preparação do mesmo, composição farmacêutica. | |
| CN103501782A (zh) | 黄斑变性预防或治疗用药物组合物 | |
| TWI708764B (zh) | 一種雄性激素受體抑制劑的結晶形式及其製備方法 | |
| CN101209994B (zh) | 选择性m4受体拮抗剂及其医药用途 | |
| TWI809330B (zh) | Cdk9抑制劑的多晶型物及其製法和用途 | |
| TWI659041B (zh) | 類固醇樣化合物之多晶型形式以及其製備方法及用途 | |
| TWI846516B (zh) | Cdk9抑制劑的多晶型物及其製法和用途 | |
| JP2013541588A5 (OSRAM) | ||
| CN118164965A (zh) | 嘧啶-三氮唑-氟取代苯基环丙胺衍生物及其应用 |