ATE184281T1 - 9-hydroxy-pyrido (1,2-a> pyrimidin-4-on-ether- derivate - Google Patents
9-hydroxy-pyrido (1,2-a> pyrimidin-4-on-ether- derivateInfo
- Publication number
- ATE184281T1 ATE184281T1 AT95901389T AT95901389T ATE184281T1 AT E184281 T1 ATE184281 T1 AT E184281T1 AT 95901389 T AT95901389 T AT 95901389T AT 95901389 T AT95901389 T AT 95901389T AT E184281 T1 ATE184281 T1 AT E184281T1
- Authority
- AT
- Austria
- Prior art keywords
- pct
- novel compounds
- date
- 4alkyl
- sec
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP93203270 | 1993-11-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE184281T1 true ATE184281T1 (de) | 1999-09-15 |
Family
ID=8214180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT95901389T ATE184281T1 (de) | 1993-11-23 | 1994-11-16 | 9-hydroxy-pyrido (1,2-a> pyrimidin-4-on-ether- derivate |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US5688799A (de) |
| EP (1) | EP0730594B1 (de) |
| JP (1) | JP3553951B2 (de) |
| AT (1) | ATE184281T1 (de) |
| AU (1) | AU687940B2 (de) |
| CA (1) | CA2175372C (de) |
| DE (1) | DE69420579T2 (de) |
| DK (1) | DK0730594T3 (de) |
| ES (1) | ES2137486T3 (de) |
| FI (1) | FI112483B (de) |
| GR (1) | GR3031500T3 (de) |
| RU (1) | RU2126406C1 (de) |
| SI (1) | SI0730594T1 (de) |
| WO (1) | WO1995014691A1 (de) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2141671B1 (es) * | 1997-12-26 | 2001-01-01 | Vita Invest Sa | Compuesto pirimidinico activo sobre el sistema nervioso central, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen. |
| WO2004009591A1 (en) * | 2002-07-22 | 2004-01-29 | Aurobindo Pharma Ltd. | A process for the preparation of antipsychotic risperidone |
| WO2004020439A2 (en) * | 2002-08-30 | 2004-03-11 | Sunil Sadanand Nadkarni | Improved process for preparation of risperidone |
| HUP0401379A3 (en) * | 2004-07-08 | 2006-04-28 | Richter Gedeon Vegyeszet | Process for the preparation of risperidon |
| ES2546268T3 (es) * | 2004-09-09 | 2015-09-22 | Janssen Pharmaceutica Nv | Preparación de 9-hidroxi-3-(2-hidroxietil)-2-metil-4H-pirido[1,2-a]pirimidin-4-ona y sus cristales |
| HUP0402163A2 (en) * | 2004-10-25 | 2006-05-29 | Richter Gedeon Vegyeszet | Process for the preparation of risperidone |
| ES2304336T1 (es) * | 2006-08-14 | 2008-10-16 | Teva Pharmaceutical Industries Ltd. | Formas cristalinas de 9-hidroxi-risperidona (paliperidona). |
| US7915412B2 (en) * | 2006-08-14 | 2011-03-29 | Teva Pharmaceutical Industries, Ltd. | Process for the synthesis of 9-hydroxy risperidone (paliperidone) |
| US7820816B2 (en) * | 2006-08-23 | 2010-10-26 | Teva Pharmaceutical Industries Ltd. | Process for the synthesis of CMHTP and intermediates thereof |
| CN101600716A (zh) | 2007-01-08 | 2009-12-09 | 阿特维斯集团公司 | 用于制备9-羟基-3-(2-氯乙基)-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮盐酸盐的改进方法 |
| US20080171876A1 (en) * | 2007-05-10 | 2008-07-17 | Santiago Ini | Pure paliperidone and processes for preparing thereof |
| WO2009010988A1 (en) * | 2007-07-19 | 2009-01-22 | Natco Pharma Limited | An improved, industrially viable process for the preparation of high purity paliperidone |
| EP2178872A1 (de) * | 2007-07-27 | 2010-04-28 | Synthon B.V. | Paliperidonderivate |
| PL2079446T3 (pl) * | 2007-08-21 | 2012-04-30 | Teva Pharma | Preparat paliperidonu o przedłużonym uwalnianiu |
| US20090061005A1 (en) * | 2007-08-21 | 2009-03-05 | Actavis Group Ptc Ehf | Paliperidone Polymorphs |
| WO2009044413A2 (en) * | 2007-10-05 | 2009-04-09 | Matrix Laboratories Limited | Improved process for preparing paliperidone, novel polymorphic forms of the same and process thereof |
| US20090270620A1 (en) * | 2007-11-27 | 2009-10-29 | Santiago Ini | Processes for preparing crystal forms of 9-hydroxy-risperidone (paliperidone) |
| CL2008003667A1 (es) * | 2007-12-10 | 2010-06-04 | Synthon Bv | Proceso de preparacion de etil-6,7,8,9-tetrahidro-9-hidroxi-2-metil-4h-pirido[1,2-a]piridin-4-ona; y uno de los intermediarios considerados en el proceso descrito; util en la preparacion de paliperidona. |
| TWI385157B (zh) * | 2008-01-16 | 2013-02-11 | Scinopharm Taiwan Ltd | 用於製備帕潘立酮(paliperidone)之新穎中間體 |
| WO2009116071A2 (en) * | 2008-02-05 | 2009-09-24 | Watson Pharma Private Limited | An improved process for preparation of paliperidone |
| WO2009118655A2 (en) * | 2008-03-27 | 2009-10-01 | Actavis Group Ptc Ehf | Highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity |
| ES2625323T3 (es) * | 2008-05-29 | 2017-07-19 | Inke, S.A. | Proceso para preparar paliperidona e intermedios de la misma |
| EP2300467A4 (de) | 2008-06-16 | 2012-04-25 | Msn Lab Ltd | Neuartige und verbesserte verfahren zur herstellung von paliperidon |
| US7932385B2 (en) | 2008-07-11 | 2011-04-26 | Synthon Bv | Paliperidone ketone |
| EP2321311B1 (de) * | 2008-07-11 | 2012-09-19 | Synthon B.V. | Synthese von paliperidon |
| WO2010064134A2 (en) * | 2008-12-05 | 2010-06-10 | Cadila Pharmaceuticals Ltd. | Process of synthesis of paliperidone |
| EP2202234A1 (de) | 2008-12-24 | 2010-06-30 | Laboratorios Lesvi, S.L. | Reinigung von Paliperidon |
| WO2010136895A1 (en) | 2009-05-28 | 2010-12-02 | Actavis Group Ptc Ehf | Solid state forms of paliperidone salts and process for the preparation thereof |
| EP2475663A2 (de) | 2009-09-10 | 2012-07-18 | Actavis Group Ptc Ehf | Paliperidon oder substantiell verunreinigungsfreies pharmazeutisch akzeptables salz daraus |
| WO2011073997A2 (en) * | 2009-12-14 | 2011-06-23 | Cadila Healthcare Limited | Process for preparing paliperidone and pharmaceutically acceptable salts thereof |
| US8088594B2 (en) * | 2010-03-16 | 2012-01-03 | Saladax Biomedical Inc. | Risperidone immunoassay |
| WO2012035554A1 (en) | 2010-09-14 | 2012-03-22 | Megafine Pharma (P) Ltd. | An improved process for the preparation of highly pure paliperidone |
| CN103387575A (zh) * | 2013-07-22 | 2013-11-13 | 江苏万特制药有限公司 | 帕潘立酮的制备方法及其关键中间体 |
| KR101867988B1 (ko) * | 2016-11-02 | 2018-06-15 | 주식회사 엔지켐생명과학 | 팔리페리돈 중간체 및 이를 이용한 팔리페리돈의 제조방법 |
| CN115260190A (zh) * | 2022-08-30 | 2022-11-01 | 南开大学 | 一种帕利哌酮前药、制剂及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4485107A (en) * | 1982-11-01 | 1984-11-27 | Janssen Pharmaceutica N.V. | [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones |
| US4804663A (en) * | 1985-03-27 | 1989-02-14 | Janssen Pharmaceutica N.V. | 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles |
| CA2000786C (en) * | 1988-11-07 | 1999-01-26 | Janssen Pharmaceutica, Naamloze Vennootschap | 3-piperidinyl-1,2-benzisoxazoles |
| US5158952A (en) * | 1988-11-07 | 1992-10-27 | Janssen Pharmaceutica N.V. | 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use |
| GB9008850D0 (en) * | 1990-04-19 | 1990-06-13 | Janssen Pharmaceutica Nv | Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones |
-
1994
- 1994-11-16 SI SI9430270T patent/SI0730594T1/xx not_active IP Right Cessation
- 1994-11-16 US US08/637,754 patent/US5688799A/en not_active Expired - Fee Related
- 1994-11-16 ES ES95901389T patent/ES2137486T3/es not_active Expired - Lifetime
- 1994-11-16 AU AU10654/95A patent/AU687940B2/en not_active Ceased
- 1994-11-16 EP EP95901389A patent/EP0730594B1/de not_active Expired - Lifetime
- 1994-11-16 CA CA002175372A patent/CA2175372C/en not_active Expired - Fee Related
- 1994-11-16 WO PCT/EP1994/003804 patent/WO1995014691A1/en not_active Ceased
- 1994-11-16 DK DK95901389T patent/DK0730594T3/da active
- 1994-11-16 DE DE69420579T patent/DE69420579T2/de not_active Expired - Fee Related
- 1994-11-16 JP JP51480895A patent/JP3553951B2/ja not_active Expired - Fee Related
- 1994-11-16 AT AT95901389T patent/ATE184281T1/de not_active IP Right Cessation
- 1994-11-16 RU RU96113091A patent/RU2126406C1/ru not_active IP Right Cessation
-
1996
- 1996-05-22 FI FI962155A patent/FI112483B/fi active
-
1999
- 1999-10-13 GR GR990402593T patent/GR3031500T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0730594B1 (de) | 1999-09-08 |
| GR3031500T3 (en) | 2000-01-31 |
| FI112483B (fi) | 2003-12-15 |
| AU1065495A (en) | 1995-06-13 |
| EP0730594A1 (de) | 1996-09-11 |
| JP3553951B2 (ja) | 2004-08-11 |
| DK0730594T3 (da) | 2000-03-27 |
| FI962155L (fi) | 1996-05-22 |
| CA2175372A1 (en) | 1995-06-01 |
| DE69420579D1 (de) | 1999-10-14 |
| CA2175372C (en) | 2006-02-21 |
| RU2126406C1 (ru) | 1999-02-20 |
| AU687940B2 (en) | 1998-03-05 |
| FI962155A0 (fi) | 1996-05-22 |
| SI0730594T1 (en) | 1999-12-31 |
| US5688799A (en) | 1997-11-18 |
| DE69420579T2 (de) | 2000-04-27 |
| ES2137486T3 (es) | 1999-12-16 |
| JPH09505574A (ja) | 1997-06-03 |
| WO1995014691A1 (en) | 1995-06-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| UEP | Publication of translation of european patent specification | ||
| REN | Ceased due to non-payment of the annual fee |