HUP0500109A3 - Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones - Google Patents
Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-onesInfo
- Publication number
- HUP0500109A3 HUP0500109A3 HU0500109A HUP0500109A HUP0500109A3 HU P0500109 A3 HUP0500109 A3 HU P0500109A3 HU 0500109 A HU0500109 A HU 0500109A HU P0500109 A HUP0500109 A HU P0500109A HU P0500109 A3 HUP0500109 A3 HU P0500109A3
- Authority
- HU
- Hungary
- Prior art keywords
- pyrid
- pyrazolo
- dihydro
- ones
- synthesis
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D211/86—Oxygen atoms
- C07D211/88—Oxygen atoms attached in positions 2 and 6, e.g. glutarimide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D211/86—Oxygen atoms
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US33908501P | 2001-12-10 | 2001-12-10 | |
PCT/US2002/038559 WO2003049681A2 (en) | 2001-12-10 | 2002-12-03 | Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0500109A2 HUP0500109A2 (hu) | 2005-05-30 |
HUP0500109A3 true HUP0500109A3 (en) | 2007-08-28 |
Family
ID=23327425
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0500109A HUP0500109A3 (en) | 2001-12-10 | 2002-12-03 | Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
Country Status (13)
Country | Link |
---|---|
US (3) | US6919451B2 (hu) |
EP (1) | EP1467984A4 (hu) |
JP (1) | JP2005511712A (hu) |
KR (1) | KR20040073467A (hu) |
CN (1) | CN1639147A (hu) |
AU (1) | AU2002346624A1 (hu) |
BR (1) | BR0214845A (hu) |
HU (1) | HUP0500109A3 (hu) |
IL (1) | IL161955A0 (hu) |
MX (1) | MXPA04005508A (hu) |
PL (1) | PL371930A1 (hu) |
TW (2) | TW200738672A (hu) |
WO (1) | WO2003049681A2 (hu) |
Families Citing this family (76)
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TWI331526B (en) | 2001-09-21 | 2010-10-11 | Bristol Myers Squibb Pharma Co | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
ATE544750T1 (de) * | 2001-09-21 | 2012-02-15 | Bristol Myers Squibb Co | Lactamhaltige verbindungen und ihre derivate als faktor-xa-hemmer |
US20070203178A1 (en) * | 2004-09-28 | 2007-08-30 | Malley Mary F | Crystalline solvates of apixaban |
US7396932B2 (en) * | 2004-09-28 | 2008-07-08 | Bristol-Myers Squibb Company | Process for preparing 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
US20060069085A1 (en) * | 2004-09-28 | 2006-03-30 | Rulin Zhao | Preparation of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
CN101065379B (zh) * | 2004-09-28 | 2011-05-11 | 布里斯托尔-迈尔斯斯奎布公司 | 制备4,5-二氢-吡唑并[3,4-c]吡啶-2-酮的方法 |
US7304157B2 (en) | 2004-09-28 | 2007-12-04 | Bristol-Myers Squibb Company | Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
DE102006025315A1 (de) * | 2006-05-31 | 2007-12-06 | Bayer Healthcare Ag | Tetrahydro-pyrrolopyridin-, Tetrahydro-pyrazolopyridin-, Tetrahydro-imidazopyridin- und Tetrahydro-triazolopyridin-Derivate und ihre Verwendung |
DE102007028406A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
DE102007028319A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
DE102007028407A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
DE102007032344A1 (de) * | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Prodrug-Derivate von 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-carboxamid |
US20090076069A1 (en) * | 2007-09-14 | 2009-03-19 | Protia, Llc | Deuterium-enriched apixaban |
US20100130543A1 (en) * | 2008-09-15 | 2010-05-27 | Auspex Pharmaceuticals, Inc. | Pyrazole carboxamide inhibitors of factor xa |
CN101967145B (zh) * | 2010-09-09 | 2012-07-04 | 华东理工大学 | 一种抗血栓药物阿匹沙班的制备方法 |
ITMI20111047A1 (it) * | 2011-06-10 | 2012-12-11 | Dipharma Francis Srl | Forma cristallina di apixaban |
ITMI20111135A1 (it) * | 2011-06-22 | 2012-12-23 | Dipharma Francis Srl | Procedimento per la preparazione di apixaban |
US8884016B2 (en) | 2011-06-10 | 2014-11-11 | Dipharma Francis S.R.L. | Apixaban preparation process |
CN103242310A (zh) * | 2012-02-10 | 2013-08-14 | 苏州迈泰生物技术有限公司 | 吡唑并吡啶酮类化合物及其在制备抗凝血药物中的用途 |
CN102675314A (zh) * | 2012-06-14 | 2012-09-19 | 南京正科制药有限公司 | 一种阿哌沙班的合成方法 |
CN103626759B (zh) * | 2012-08-24 | 2015-10-21 | 上海医药工业研究院 | 一种阿哌沙班的中间体的制备方法 |
WO2014072884A1 (en) * | 2012-11-12 | 2014-05-15 | Alembic Pharmaceuticals Limited | Process for the synthesis of apixaban |
CZ304846B6 (cs) | 2012-11-13 | 2014-12-03 | Zentiva, K.S. | Způsob přípravy APIXABANU |
EP2945946B1 (en) | 2013-01-17 | 2017-07-12 | Glenmark Pharmaceuticals Limited | Process for the preparation and purification of apixaban |
CN103539795A (zh) * | 2013-03-18 | 2014-01-29 | 齐鲁制药有限公司 | 阿哌沙班的多晶型及其制备方法 |
CN104109165A (zh) * | 2013-04-19 | 2014-10-22 | 四川海思科制药有限公司 | 4,5-二氢-吡唑并[3,4-c]吡啶-2-酮衍生物、其制备方法以及应用 |
CZ2013305A3 (cs) | 2013-04-23 | 2014-11-05 | Zentiva, K.S. | Nové krystalické formy APIXABANU a způsob jejich přípravy |
WO2014203275A2 (en) | 2013-06-18 | 2014-12-24 | Cadila Healthcare Limited | An improved process for the preparation of apixaban and intermediates thereof |
CN103739541B (zh) * | 2014-01-07 | 2016-01-20 | 上海现代制药股份有限公司 | 5,6-二氢-3-(4-吗啉基)-1-[4-(2-氧代-1-哌啶基)苯基]-2(1h)-吡啶酮的制备方法 |
IN2014MU00197A (hu) | 2014-01-21 | 2015-08-28 | Wanbury Ltd | |
CN103896940B (zh) * | 2014-03-25 | 2016-02-03 | 江苏弘和药物研发有限公司 | 一种阿哌沙班的合成方法 |
CN103923080B (zh) * | 2014-04-04 | 2016-06-22 | 苏州景泓生物技术有限公司 | 一种制备抗血栓药物阿哌沙班的方法 |
CN104045637B (zh) * | 2014-04-18 | 2016-04-06 | 河北科技大学 | 一种阿哌沙班的制备方法 |
WO2015162551A1 (en) | 2014-04-21 | 2015-10-29 | Mylan Laboratories Ltd | Process for the preparation of apixaban |
KR102412045B1 (ko) * | 2014-05-22 | 2022-06-22 | 놀스 차이나 파마수티칼 컴퍼니., 엘티디. | 혈액응고인자 Xa 억제제로서의 히드라지드 화합물 |
WO2015177801A1 (en) * | 2014-05-23 | 2015-11-26 | Symed Labs Limited | Novel process for the preparation of a lactam-containing compound |
HU231122B1 (hu) | 2014-08-06 | 2020-11-30 | Egis Gyógyszergyár Zrt | Eljárás apixaban előállítására |
DK3180335T3 (da) | 2014-08-11 | 2021-08-09 | Angion Biomedica Corp | Cytokrom-p450-inhibitorer og anvendelser deraf |
CN104311555B (zh) * | 2014-09-19 | 2016-04-20 | 广东东阳光药业有限公司 | 吡唑并哌啶酮类化合物及其组合物及用途 |
CN104327074B (zh) * | 2014-09-19 | 2016-01-06 | 广东东阳光药业有限公司 | 含有内酰胺取代基的吡唑并哌啶酮类化合物及其组合物及用途 |
CN104311558B (zh) * | 2014-09-19 | 2016-06-01 | 广东东阳光药业有限公司 | 含有环己烷取代基的吡唑并哌啶酮类化合物及其组合物及用途 |
CN104277037B (zh) * | 2014-09-19 | 2015-12-09 | 广东东阳光药业有限公司 | 含有螺环的吡唑并哌啶酮类化合物及其组合物及用途 |
CN104277040B (zh) * | 2014-09-19 | 2016-04-20 | 广东东阳光药业有限公司 | 含有酰基哌嗪酮取代基的吡唑并哌啶酮类化合物及其组合物及用途 |
EP3009435B1 (en) * | 2014-10-15 | 2016-08-17 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Apixaban glycol esters as key intermediates and impurities of the synthesis of Apixaban |
WO2016067308A1 (en) | 2014-10-28 | 2016-05-06 | Jubilant Generics Limited (Formerly Jubilant Life Sciences Division) | Process for the preparation of apixaban and intermediates thereof |
HU230991B1 (hu) * | 2014-11-19 | 2019-08-28 | Egis Gyógyszergyár Zrt. | Eljárás és köztitermék apixaban előállítására |
US9603846B2 (en) | 2014-11-25 | 2017-03-28 | Cadila Healthcare Limited | Process for the preparation of apixaban |
WO2016109492A1 (en) | 2014-12-31 | 2016-07-07 | Angion Biomedica Corp | Methods and agents for treating disease |
CN104892601B (zh) * | 2015-06-09 | 2017-09-19 | 江苏中邦制药有限公司 | 一种抗血栓药物阿哌沙班的制备方法 |
EP3064497A1 (en) * | 2015-07-20 | 2016-09-07 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Dimer impurities of apixaban and method to remove them |
CN106632312B (zh) * | 2015-11-03 | 2019-05-14 | 上海医药工业研究院 | 一种阿哌沙班有关物质、中间体、制备方法及其应用 |
CN105732618A (zh) * | 2016-02-02 | 2016-07-06 | 扬州大学 | 一种合成4-(2-氧代哌啶-1-基)芳基羧酸乙酯类化合物的方法 |
ES2827459T3 (es) * | 2016-04-04 | 2021-05-21 | Zakl Farmaceutyczne Polpharma Sa | Procedimiento para la preparación de apixaban |
US10077263B2 (en) * | 2016-04-29 | 2018-09-18 | Optimus Drugs Private Limited | Process for the preparation of Apixaban |
CN106117200B (zh) * | 2016-06-27 | 2018-02-02 | 张士伟 | 预防或治疗关节置换静脉血栓药物阿哌沙班的制备方法 |
WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
US20180072741A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyrimidine compounds and uses thereof |
CN115819417A (zh) | 2016-09-09 | 2023-03-21 | 因赛特公司 | 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途 |
CN107434806A (zh) * | 2016-12-09 | 2017-12-05 | 陕西科技大学 | 一种阿哌沙班羧酸衍生物的γ晶型固体物质及其制备方法与用途 |
US20180228786A1 (en) | 2017-02-15 | 2018-08-16 | Incyte Corporation | Pyrazolopyridine compounds and uses thereof |
US10722495B2 (en) | 2017-09-08 | 2020-07-28 | Incyte Corporation | Cyanoindazole compounds and uses thereof |
CN107955002B (zh) * | 2017-12-27 | 2019-12-24 | 上海博志研新药物技术有限公司 | 阿哌沙班及其中间体的制备方法 |
CN107955003A (zh) * | 2017-12-28 | 2018-04-24 | 河北常山生化药业股份有限公司 | 一种阿哌沙班中间体2合成过程中特定杂质s4的清除方法 |
CN107936015B (zh) * | 2017-12-28 | 2020-05-12 | 浙江天宇药业股份有限公司 | 一种n-1晶型的阿哌沙班的合成方法 |
US10745388B2 (en) | 2018-02-20 | 2020-08-18 | Incyte Corporation | Indazole compounds and uses thereof |
WO2019164847A1 (en) | 2018-02-20 | 2019-08-29 | Incyte Corporation | Indazole compounds and uses thereof |
PL3755703T3 (pl) | 2018-02-20 | 2022-11-07 | Incyte Corporation | Pochodne n-(fenylo)-2-(fenylo)pirymidyno-4-karboksyamidu i związki pokrewne jako inhibitory hpk1 do leczenia nowotworu |
US11299473B2 (en) | 2018-04-13 | 2022-04-12 | Incyte Corporation | Benzimidazole and indole compounds and uses thereof |
US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
EP3856348B1 (en) | 2018-09-25 | 2024-01-03 | Incyte Corporation | Pyrazolo[4,3-d]pyrimidine compounds as alk2 and/or fgfr modulators |
KR102188341B1 (ko) | 2018-10-24 | 2020-12-08 | 하나제약 주식회사 | 아픽사반의 제조방법 |
AU2020326703A1 (en) | 2019-08-06 | 2022-02-17 | Incyte Corporation | Solid forms of an HPK1 inhibitor |
CN111253392B (zh) * | 2019-12-17 | 2021-06-11 | 哈尔滨珍宝制药有限公司 | 一种制备阿哌沙班的方法 |
CN113214142B (zh) * | 2020-01-21 | 2024-01-30 | 浙江九洲药业股份有限公司 | 一种阿哌沙班的中间体及制备方法 |
JP2022022550A (ja) * | 2020-06-26 | 2022-02-07 | ダイト株式会社 | アピキサバンの新規製造方法 |
CN112142736B (zh) * | 2020-10-29 | 2021-08-10 | 怀化学院 | 一种阿哌沙班杂质1的制备方法 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2459240A1 (fr) | 1979-06-21 | 1981-01-09 | Cm Ind | Aminopiperidines anorexigenes, procede pour leur preparation, intermediaires dans ledit procede et medicaments qui les contiennent |
CN100340559C (zh) | 1998-12-23 | 2007-10-03 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为凝血因子xa抑制剂的含氮杂双环 |
US6329527B1 (en) | 1999-10-21 | 2001-12-11 | Bristol-Myers Squibb Pharma Company | Synthesis of 1,3,5-trisubstituted pyrazoles |
TWI331526B (en) | 2001-09-21 | 2010-10-11 | Bristol Myers Squibb Pharma Co | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
ATE544750T1 (de) * | 2001-09-21 | 2012-02-15 | Bristol Myers Squibb Co | Lactamhaltige verbindungen und ihre derivate als faktor-xa-hemmer |
US7304157B2 (en) * | 2004-09-28 | 2007-12-04 | Bristol-Myers Squibb Company | Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
US7396932B2 (en) * | 2004-09-28 | 2008-07-08 | Bristol-Myers Squibb Company | Process for preparing 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
US20060069085A1 (en) * | 2004-09-28 | 2006-03-30 | Rulin Zhao | Preparation of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
-
2002
- 2002-11-20 TW TW096118206A patent/TW200738672A/zh unknown
- 2002-11-20 TW TW091133820A patent/TW200303201A/zh unknown
- 2002-12-03 CN CNA028242920A patent/CN1639147A/zh active Pending
- 2002-12-03 WO PCT/US2002/038559 patent/WO2003049681A2/en active Application Filing
- 2002-12-03 AU AU2002346624A patent/AU2002346624A1/en not_active Abandoned
- 2002-12-03 JP JP2003550732A patent/JP2005511712A/ja not_active Withdrawn
- 2002-12-03 BR BR0214845-5A patent/BR0214845A/pt not_active IP Right Cessation
- 2002-12-03 HU HU0500109A patent/HUP0500109A3/hu unknown
- 2002-12-03 IL IL16195502A patent/IL161955A0/xx unknown
- 2002-12-03 MX MXPA04005508A patent/MXPA04005508A/es not_active Application Discontinuation
- 2002-12-03 US US10/308,741 patent/US6919451B2/en not_active Expired - Fee Related
- 2002-12-03 EP EP02784699A patent/EP1467984A4/en not_active Withdrawn
- 2002-12-03 KR KR10-2004-7008884A patent/KR20040073467A/ko not_active Application Discontinuation
- 2002-12-03 PL PL02371930A patent/PL371930A1/xx not_active Application Discontinuation
-
2005
- 2005-06-08 US US11/147,634 patent/US7153960B2/en not_active Expired - Fee Related
-
2006
- 2006-09-07 US US11/470,741 patent/US20070027186A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
EP1467984A2 (en) | 2004-10-20 |
US20030181466A1 (en) | 2003-09-25 |
TW200738672A (en) | 2007-10-16 |
IL161955A0 (en) | 2005-11-20 |
BR0214845A (pt) | 2004-12-07 |
JP2005511712A (ja) | 2005-04-28 |
KR20040073467A (ko) | 2004-08-19 |
TW200303201A (en) | 2003-09-01 |
HUP0500109A2 (hu) | 2005-05-30 |
WO2003049681A2 (en) | 2003-06-19 |
EP1467984A4 (en) | 2005-12-07 |
US7153960B2 (en) | 2006-12-26 |
MXPA04005508A (es) | 2004-12-06 |
WO2003049681A3 (en) | 2003-09-18 |
US6919451B2 (en) | 2005-07-19 |
PL371930A1 (en) | 2005-07-11 |
US20070027186A1 (en) | 2007-02-01 |
AU2002346624A1 (en) | 2003-06-23 |
CN1639147A (zh) | 2005-07-13 |
US20050245566A1 (en) | 2005-11-03 |
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