AR070924A1 - Formas cristalinas y dos formas solvatadas de sales del acido lactico de 4- amino -5- fluoro-3-(5-(4-metilpiperazin-1-il ) -1h- bencimidazol-2-il) quinolin -2-(1h) - ona - Google Patents
Formas cristalinas y dos formas solvatadas de sales del acido lactico de 4- amino -5- fluoro-3-(5-(4-metilpiperazin-1-il ) -1h- bencimidazol-2-il) quinolin -2-(1h) - onaInfo
- Publication number
- AR070924A1 AR070924A1 ARP090100957A ARP090100957A AR070924A1 AR 070924 A1 AR070924 A1 AR 070924A1 AR P090100957 A ARP090100957 A AR P090100957A AR P090100957 A ARP090100957 A AR P090100957A AR 070924 A1 AR070924 A1 AR 070924A1
- Authority
- AR
- Argentina
- Prior art keywords
- quinolin
- amino
- lactic acid
- substantially pure
- fluoro
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Abstract
Formas cristalinas o polimorfos de sales del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1H-bencimidazol-2-il]quinolin-2(1H)-ona, composiciones farmacéuticas que las comprenden y métodos de tratamiento que las utilizan. Los compuestos son utiles para tratar cáncer de diversos organos, linfomas, leucemias y carcinoma de células pequenas. Reivindicacion 1: Una forma cristalina anhidra II sustancialmente pura de la sal del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1H-bencimidazol-2-il]quinolin-2(1H)-ona caracterizada por una configuracion de difraccion de rayos X de polvo que muestra una máxima característica a 18,5 grados, 2 theta. Reivindicacion 2: Una forma cristalina anhidra II sustancialmente pura de la sal del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il-1H-bencimidazol-2-il]quinolin-2(1H)-ona caracterizada por la configuracion de difraccion de rayos X de polvo que se muestra en la Figura 1. Reivindicacion 3: La forma cristalina sustancialmente pura de acuerdo con la reivindicacion 2, en donde la configuracion de difraccion de rayos X de polvo muestra máximas características a 8,2, 11,8, 12,9, 13,8, 14,7, 16,6, 18,5, 20,3, 23,5 grados, 2 theta. Reivindicacion 4: Una forma cristalina hemipentahidrato sustancialmente pura de la sal del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1H-bencimidazol-2-il]quinolin-2(1H)-ona caracterizada por la configuracion de difraccion de rayos X de polvo que muestra una máxima característica a 22,5 grados, 2 theta. Reivindicacion 5: Una forma cristalina hemipentahidrato sustancialmente pura de la sal del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1H-bencimidazol-2-il]quinolin-2(1H)-ona caracterizada por la configuracion de difraccion de rayos X de polvo que se muestra en la Figura 2. Reivindicacion 6: La forma cristalina sustancialmente pura de acuerdo con la reivindicacion 5, en donde la configuracion de difraccion de rayos X de polvo muestra máximas características a 6,8, 9,3, 12,1, 12,7, 13,1, 13,4, 16,5, 17,3, 18,7, 19,3, 19,8, 20,4, 22,5, 23,3, 25,8, 26,2, 27,1 grados, 2 theta. Reivindicacion 7: Una forma cristalina metanol-solvato sustancialmente pura de la sal del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1H-bencimidazol-2-il]quinolin-2(1H)-ona caracterizada por la configuracion de difraccion de rayos X de polvo que muestra una máxima característica a 19,5 grados, 2 theta. Reivindicacion 8: Una forma cristalina metanol-solvato sustancialmente pura de la sal del ácido láctico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1H-bencimidazol-2-il]quinolin-2(1H)-ona caracterizada por la configuracion de difraccion de rayos X de polvo que se muestra en la Figura 3. Reivindicacion 9: La forma cristalina sustancialmente pura de acuerdo con la reivindicacion 8, en donde la configuracion de difraccion de rayos X de polvo muestra máximas características a 6,5, 9,4, 11,9, 12,2, 18,0, 19,5, 22,5, 24,0, 26,3 grados, 2 theta.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US3774608P | 2008-03-19 | 2008-03-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR070924A1 true AR070924A1 (es) | 2010-05-12 |
Family
ID=40622140
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090100957A AR070924A1 (es) | 2008-03-19 | 2009-03-17 | Formas cristalinas y dos formas solvatadas de sales del acido lactico de 4- amino -5- fluoro-3-(5-(4-metilpiperazin-1-il ) -1h- bencimidazol-2-il) quinolin -2-(1h) - ona |
Country Status (25)
Country | Link |
---|---|
US (1) | US8563556B2 (es) |
EP (1) | EP2257544B1 (es) |
JP (1) | JP2011515370A (es) |
KR (1) | KR20100137517A (es) |
CN (1) | CN101970425B (es) |
AR (1) | AR070924A1 (es) |
AU (1) | AU2009227003B2 (es) |
BR (1) | BRPI0909762A2 (es) |
CA (1) | CA2718076A1 (es) |
CL (1) | CL2009000651A1 (es) |
CO (1) | CO6321253A2 (es) |
EC (1) | ECSP10010555A (es) |
HK (1) | HK1147492A1 (es) |
IL (1) | IL208020A0 (es) |
MA (1) | MA32230B1 (es) |
MX (1) | MX2010010152A (es) |
MY (1) | MY150554A (es) |
NZ (2) | NZ600887A (es) |
PE (1) | PE20091628A1 (es) |
PH (2) | PH12012502568A1 (es) |
RU (1) | RU2497820C2 (es) |
SG (1) | SG188919A1 (es) |
TW (1) | TWI426072B (es) |
WO (1) | WO2009115562A2 (es) |
ZA (1) | ZA201006263B (es) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PE20091628A1 (es) | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
PL2558095T3 (pl) | 2010-04-16 | 2019-06-28 | Novartis Ag | Związek organiczny, przeznaczony do stosowania w leczeniu raka wątroby |
RU2012148706A (ru) | 2010-04-16 | 2014-05-27 | Новартис Аг | Комбинация органичемких соединений |
UY33472A (es) | 2010-06-30 | 2012-01-31 | Novartis Ag | ?composiciones farmacéuticas que comprenden monohidrato de lactato de 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1hbencimidazol-2-il]-1h-quinolin-2-ona?. |
RU2013146242A (ru) | 2011-03-17 | 2015-04-27 | Новартис Аг | Fgfr и его лиганды в качестве биомаркеров рака молочной железы у hr-положительных индивидуумов |
EP2709729A1 (en) | 2011-05-19 | 2014-03-26 | Novartis AG | 4-amino-5-fluoro-3- [6- (4 -methylpiperazin- 1 - yl) - 1h - benzimidazol - 2 - yl]- 1h - quinoli n-2-one for use in the treatment of adenoid cystic carcinoma |
EP2755655A1 (en) | 2011-09-15 | 2014-07-23 | Novartis AG | Use of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one in the treatment of cancer in moderate hepatic impaired patients |
WO2013063003A1 (en) | 2011-10-28 | 2013-05-02 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
WO2013116293A1 (en) | 2012-01-31 | 2013-08-08 | Novartis Ag | Combination of a rtk inhibitor with an anti - estrogen and use thereof for the treatment of cancer |
WO2014011284A1 (en) | 2012-07-11 | 2014-01-16 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
WO2014058785A1 (en) | 2012-10-10 | 2014-04-17 | Novartis Ag | Combination therapy |
EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
PT3116909T (pt) | 2014-03-14 | 2020-01-30 | Novartis Ag | Moléculas de anticorpos para lag-3 e suas utilizações |
MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
TN2017000129A1 (en) | 2014-10-14 | 2018-10-19 | Dana Farber Cancer Inst Inc | Antibody molecules to pd-l1 and uses thereof |
US20170340733A1 (en) | 2014-12-19 | 2017-11-30 | Novartis Ag | Combination therapies |
CN107530415A (zh) | 2015-03-10 | 2018-01-02 | 艾杜罗生物科技公司 | 用于活化“干扰素基因刺激物”依赖性信号传导的组合物和方法 |
LT3317301T (lt) | 2015-07-29 | 2021-07-26 | Novartis Ag | Kombinuotos terapijos, apimančios antikūno molekules prieš lag-3 |
US20180207273A1 (en) | 2015-07-29 | 2018-07-26 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
MA43186B1 (fr) | 2015-11-03 | 2022-03-31 | Janssen Biotech Inc | Anticorps se liant spécifiquement à pd-1 et leurs utilisations |
CA3007671A1 (en) | 2015-12-17 | 2017-06-22 | Novartis Ag | Antibody molecules to pd-1 and uses thereof |
US11098077B2 (en) | 2016-07-05 | 2021-08-24 | Chinook Therapeutics, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
Family Cites Families (13)
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BRPI0113757B8 (pt) * | 2000-09-11 | 2017-11-07 | Chiron Corp | derivados de quinolinona como inibidores de tirosina quinase |
US20050256157A1 (en) * | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
EP2573079A3 (en) * | 2002-08-23 | 2015-03-11 | Novartis AG | Benzimidazole quinolinones and uses thereof |
US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
WO2004043389A2 (en) * | 2002-11-13 | 2004-05-27 | Chiron Corporation | Methods of treating cancer and related methods |
CN100377709C (zh) * | 2002-11-13 | 2008-04-02 | 希龙公司 | 受体酪氨酸激酶抑制剂的制药用途及相关检测方法 |
WO2005046590A2 (en) * | 2003-11-07 | 2005-05-26 | Chiron Corporation | Methods for synthesizing quinolinone compounds |
JP5019884B2 (ja) * | 2004-02-20 | 2012-09-05 | ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド | 炎症プロセスおよび転移プロセスの調節 |
KR101387985B1 (ko) * | 2005-01-27 | 2014-04-25 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 전이 종양의 치료 |
EP2270000B1 (en) * | 2005-05-23 | 2015-07-29 | Novartis AG | Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts |
CN102670530A (zh) * | 2005-11-29 | 2012-09-19 | 诺瓦提斯公司 | 喹啉酮类的制剂 |
US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
PE20091628A1 (es) | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
-
2009
- 2009-03-17 PE PE2009000395A patent/PE20091628A1/es not_active Application Discontinuation
- 2009-03-17 AR ARP090100957A patent/AR070924A1/es unknown
- 2009-03-18 CN CN200980108402.0A patent/CN101970425B/zh not_active Expired - Fee Related
- 2009-03-18 NZ NZ600887A patent/NZ600887A/xx not_active IP Right Cessation
- 2009-03-18 US US12/922,213 patent/US8563556B2/en not_active Expired - Fee Related
- 2009-03-18 WO PCT/EP2009/053222 patent/WO2009115562A2/en active Application Filing
- 2009-03-18 RU RU2010142396/04A patent/RU2497820C2/ru not_active IP Right Cessation
- 2009-03-18 BR BRPI0909762A patent/BRPI0909762A2/pt not_active IP Right Cessation
- 2009-03-18 EP EP09721534.7A patent/EP2257544B1/en active Active
- 2009-03-18 SG SG2013020011A patent/SG188919A1/en unknown
- 2009-03-18 CA CA2718076A patent/CA2718076A1/en not_active Abandoned
- 2009-03-18 MX MX2010010152A patent/MX2010010152A/es not_active Application Discontinuation
- 2009-03-18 MY MYPI20104156 patent/MY150554A/en unknown
- 2009-03-18 TW TW098108804A patent/TWI426072B/zh not_active IP Right Cessation
- 2009-03-18 NZ NZ587829A patent/NZ587829A/xx not_active IP Right Cessation
- 2009-03-18 CL CL2009000651A patent/CL2009000651A1/es unknown
- 2009-03-18 AU AU2009227003A patent/AU2009227003B2/en not_active Ceased
- 2009-03-18 JP JP2011500221A patent/JP2011515370A/ja active Pending
- 2009-03-18 KR KR1020107023196A patent/KR20100137517A/ko not_active Application Discontinuation
-
2010
- 2010-09-01 ZA ZA2010/06263A patent/ZA201006263B/en unknown
- 2010-09-06 IL IL208020A patent/IL208020A0/en not_active IP Right Cessation
- 2010-10-15 MA MA33250A patent/MA32230B1/fr unknown
- 2010-10-19 CO CO10129430A patent/CO6321253A2/es not_active Application Discontinuation
- 2010-10-19 EC EC2010010555A patent/ECSP10010555A/es unknown
-
2011
- 2011-02-18 HK HK11101661.3A patent/HK1147492A1/xx not_active IP Right Cessation
-
2012
- 2012-12-26 PH PH12012502568A patent/PH12012502568A1/en unknown
- 2012-12-26 PH PH12012502569A patent/PH12012502569A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
CA2718076A1 (en) | 2009-09-24 |
TWI426072B (zh) | 2014-02-11 |
PH12012502569A1 (en) | 2015-09-21 |
CN101970425B (zh) | 2014-04-16 |
MX2010010152A (es) | 2010-10-25 |
CL2009000651A1 (es) | 2010-07-19 |
MA32230B1 (fr) | 2011-04-01 |
CN101970425A (zh) | 2011-02-09 |
TW201000463A (en) | 2010-01-01 |
HK1147492A1 (en) | 2011-08-12 |
IL208020A0 (en) | 2010-12-30 |
RU2497820C2 (ru) | 2013-11-10 |
PH12012502568A1 (en) | 2014-10-27 |
JP2011515370A (ja) | 2011-05-19 |
PE20091628A1 (es) | 2009-11-19 |
BRPI0909762A2 (pt) | 2018-04-03 |
NZ600887A (en) | 2013-10-25 |
AU2009227003A1 (en) | 2009-09-24 |
EP2257544B1 (en) | 2014-12-03 |
MY150554A (en) | 2014-01-30 |
ECSP10010555A (es) | 2010-11-30 |
ZA201006263B (en) | 2011-05-25 |
US20110021536A1 (en) | 2011-01-27 |
SG188919A1 (en) | 2013-04-30 |
NZ587829A (en) | 2012-08-31 |
AU2009227003B2 (en) | 2013-03-14 |
RU2010142396A (ru) | 2012-04-27 |
WO2009115562A2 (en) | 2009-09-24 |
WO2009115562A3 (en) | 2009-11-26 |
US8563556B2 (en) | 2013-10-22 |
EP2257544A2 (en) | 2010-12-08 |
KR20100137517A (ko) | 2010-12-30 |
CO6321253A2 (es) | 2011-09-20 |
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