DK169923B1 - 3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse - Google Patents
3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse Download PDFInfo
- Publication number
- DK169923B1 DK169923B1 DK551989A DK551989A DK169923B1 DK 169923 B1 DK169923 B1 DK 169923B1 DK 551989 A DK551989 A DK 551989A DK 551989 A DK551989 A DK 551989A DK 169923 B1 DK169923 B1 DK 169923B1
- Authority
- DK
- Denmark
- Prior art keywords
- formula
- compounds
- alkyl
- alk
- parts
- Prior art date
Links
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
- A61P25/00—Drugs for disorders of the nervous 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US26785788A | 1988-11-07 | 1988-11-07 | |
US26785788 | 1988-11-07 |
Publications (3)
Publication Number | Publication Date |
---|---|
DK551989D0 DK551989D0 (da) | 1989-11-06 |
DK551989A DK551989A (da) | 1990-05-08 |
DK169923B1 true DK169923B1 (da) | 1995-04-03 |
Family
ID=23020416
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK551989A DK169923B1 (da) | 1988-11-07 | 1989-11-06 | 3-[[4-(1,2-benzisoxazol-3-yl)-1-piperidinyl]alkyl]-6,7,8,9-tetrahydro-2-alkyl-4H-pyrido[1,2-a]pyrimidin-4-on-forbindelser, fremgangsmåde til fremstilling deraf og antipsykotiske præparater indeholdende disse |
Country Status (21)
Country | Link |
---|---|
EP (1) | EP0368388B1 (el) |
JP (1) | JP2758045B2 (el) |
KR (1) | KR0146053B1 (el) |
AT (1) | ATE122349T1 (el) |
AU (1) | AU614437B2 (el) |
CA (1) | CA2000786C (el) |
CL (1) | CL43432B (el) |
CY (2) | CY1926A (el) |
DE (2) | DE68922577T2 (el) |
DK (1) | DK169923B1 (el) |
ES (1) | ES2075036T3 (el) |
FI (1) | FI92201C (el) |
HK (1) | HK131696A (el) |
IE (1) | IE66370B1 (el) |
IL (1) | IL92208A0 (el) |
LU (1) | LU91362I2 (el) |
NL (1) | NL300298I2 (el) |
NO (2) | NO173015C (el) |
NZ (1) | NZ231062A (el) |
PT (1) | PT92206B (el) |
ZA (1) | ZA898436B (el) |
Families Citing this family (61)
Publication number | Priority date | Publication date | Assignee | Title |
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GB9008850D0 (en) * | 1990-04-19 | 1990-06-13 | Janssen Pharmaceutica Nv | Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones |
JPH07502268A (ja) * | 1991-11-27 | 1995-03-09 | ノボ ノルディスク アクティーゼルスカブ | 化学化合物、それらの製法および使用 |
US5378714A (en) * | 1991-11-27 | 1995-01-03 | Novo Nordisk A/S | Antipsychotic piperidine derivatives |
ES2050069B1 (es) * | 1992-07-10 | 1994-12-16 | Vita Invest Sa | Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona. |
DK60593D0 (da) * | 1993-05-26 | 1993-05-26 | Novo Nordisk As | Kemiske forbindelser, deres fremstilling og anvendelse |
DK60793D0 (da) * | 1993-05-26 | 1993-05-26 | Novo Nordisk As | Kemiske forbindelser, deres fremstilling og anvendelse |
ES2236700T3 (es) * | 1993-11-19 | 2005-07-16 | Janssen Pharmaceutica N.V. | 1,2-benzazoles microencapsulados. |
AU687940B2 (en) * | 1993-11-23 | 1998-03-05 | Janssen Pharmaceutica N.V. | Novel 9-hydroxy-pyrido(1,2-a)pyrimidin-4-one ether derivatives |
ES2085234B1 (es) * | 1994-02-24 | 1997-01-16 | Vita Invest Sa | Agente activo sobre el sistema nervioso central, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen. |
TW487572B (en) * | 1996-05-20 | 2002-05-21 | Janssen Pharmaceutica Nv | Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters |
US6028083A (en) * | 1997-07-25 | 2000-02-22 | Hoechst Marion Roussel, Inc. | Esters of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol |
UA72189C2 (uk) * | 1997-11-17 | 2005-02-15 | Янссен Фармацевтика Н.В. | Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот |
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. |
AU3900499A (en) * | 1998-05-18 | 1999-12-06 | Sepracor, Inc. | (+)-hydroxyrisperidone compositions and methods |
WO1999059589A1 (en) * | 1998-05-18 | 1999-11-25 | Sepracor Inc. | (-)-hydroxyrisperidone compositions and methods |
US6342488B1 (en) | 1998-08-18 | 2002-01-29 | Sepracor, Inc. | Phosphonorisperidone and sulforisperidone compositions and methods |
ES2197801B1 (es) | 2002-03-05 | 2005-03-16 | Ferrer Internacional,S.A | Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona. |
KR20040025224A (ko) * | 2002-09-18 | 2004-03-24 | 주식회사 대웅 | 2-(2-메틸-4-옥소-6,7,8,9-테트라하이드로-4H-피리도[1,2-a]피리미딘-3-일)아세트알데히드 및 그 제조방법 |
EP1560814A1 (en) | 2002-11-13 | 2005-08-10 | Synthon B.V. | Process for making risperidone and intermediates therefor |
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 |
US20070197591A1 (en) | 2005-12-12 | 2007-08-23 | Sandra Boom | Use of paliperidone for the treatment of a mental disorder in a psychiatric patient with reduced hepatic function |
EP2133352A3 (en) * | 2006-08-14 | 2010-01-13 | Teva Pharmaceutical Industries Ltd. | Crystal form of 9-hydroxy-risperidone (paliperidone) |
EP1940834A2 (en) | 2006-08-14 | 2008-07-09 | Teva Pharmaceutical Industries Ltd. | Amorphous and crystalline forms of 9-hydroxy-risperidone (paliperidone) |
EP2133351A3 (en) * | 2006-08-14 | 2010-01-13 | Teva Pharmaceutical Industries Ltd. | Crystal form 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 |
JP2009524574A (ja) * | 2006-08-23 | 2009-07-02 | テバ ファーマシューティカル インダストリーズ リミティド | Cmhtp及びその中間体の合成方法 |
WO2008087557A2 (en) * | 2007-01-08 | 2008-07-24 | Actavis Group Ptc Ehf | An improved process for preparation of 9-hydroxy-3-(2-chloroethyl)- 2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one hydrochloride |
DK2154138T3 (en) * | 2007-04-19 | 2015-11-02 | Youxin Li | Novel compounds for the treatment of psychotic disorders, methods of preparation and uses thereof |
WO2009010988A1 (en) * | 2007-07-19 | 2009-01-22 | Natco Pharma Limited | An improved, industrially viable process for the preparation of high purity paliperidone |
US20090036470A1 (en) * | 2007-07-27 | 2009-02-05 | Jiri Bartl | Paliperidone derivatives |
WO2009045489A2 (en) * | 2007-10-03 | 2009-04-09 | Teva Pharmaceutical Industries Ltd. | Process for the synthesis of cmhtp, a paliperidone intermediate |
US8242269B2 (en) | 2007-10-09 | 2012-08-14 | Cipla Limited | Processes for the preparation of paliperidone and pharmaceutically acceptable salts thereof and intermediates for use in the processes |
US7977480B2 (en) | 2007-12-10 | 2011-07-12 | Synthon Bv | Synthesis of paliperidone |
AU2009227507A1 (en) * | 2008-02-05 | 2009-09-24 | Watson Pharma Private Limited | An improved process for preparation of paliperidone |
WO2009130710A2 (en) * | 2008-04-21 | 2009-10-29 | Glenmark Generics Limited | A process for the preparation of paliperidone intermediates |
EP2303877B1 (en) | 2008-05-29 | 2017-02-15 | Inke, S.A. | Process to prepare paliperidone and intermediates thereof |
US8481729B2 (en) | 2008-06-16 | 2013-07-09 | Msn Laboratories Limited | Processes for the preparation of paliperidone |
WO2010003702A1 (en) * | 2008-07-11 | 2010-01-14 | Synthon B.V. | Synthesis of paliperidone |
EP2318405A2 (en) | 2008-07-11 | 2011-05-11 | Synthon B.V. | Paliperidone ketone |
SI22856A (sl) * | 2008-07-31 | 2010-02-26 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Proces za pripravo paliperidona |
EP2161019A1 (en) | 2008-09-05 | 2010-03-10 | KRKA, D.D., Novo Mesto | Prolonged release multiparticulate pharmaceutical composition comprising paliperidone |
EP2199293A1 (en) | 2008-12-22 | 2010-06-23 | Chemo Ibérica, S.A. | One-step process for preparing paliperidone and its oxalate salt |
EP2202234A1 (en) | 2008-12-24 | 2010-06-30 | Laboratorios Lesvi, S.L. | Purification of paliperidone |
SI2275423T1 (sl) | 2009-07-13 | 2012-06-29 | Krka D.D., Novo Mesto | Postopek za sintezo paliperidona |
WO2011018246A2 (en) | 2009-08-13 | 2011-02-17 | Synthon B.V. | Controlled release paliperidone composition |
EP2343296A1 (en) | 2009-12-01 | 2011-07-13 | Chemo Ibérica, S.A. | A process for the purification of paliperidone |
WO2011074017A1 (en) * | 2009-12-17 | 2011-06-23 | Alkem Laboratories Ltd. | A novel process for the preparation of paliperidone |
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 |
CA2818025A1 (en) | 2010-11-15 | 2012-05-24 | Agenebio, Inc. | Pyridazine derivatives, compositions and methods for treating cognitive impairment |
CN102153552B (zh) * | 2011-03-01 | 2012-08-22 | 吉林大学 | 两种帕潘立酮药物共晶及其制备方法 |
CN102206210B (zh) * | 2011-04-01 | 2014-07-02 | 常州市第四制药厂有限公司 | 一种6-氟-3-(4-哌啶基)-1,2-苯并异噁唑盐酸盐的生产方法 |
EP2919788A4 (en) | 2012-11-14 | 2016-05-25 | Univ Johns Hopkins | METHODS AND COMPOSITIONS FOR THE TREATMENT OF SCHIZOPHRENIA |
EP3083569B1 (en) | 2013-12-20 | 2022-01-26 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
WO2016205739A1 (en) | 2015-06-19 | 2016-12-22 | Belew Mekonnen | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
BR112019012821A2 (pt) | 2016-12-19 | 2019-11-26 | Agenebio Inc | derivados de benzodiazepina, composições e métodos para o tratamento do comprometimento cognitivo |
US20180170941A1 (en) | 2016-12-19 | 2018-06-21 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
WO2019162746A1 (en) * | 2018-02-21 | 2019-08-29 | Zenvision Pharma Llp | Novel derivatives of paliperidone and process for the preparation thereof |
CN112601749B (zh) | 2018-06-19 | 2024-03-26 | 艾吉因生物股份有限公司 | 用于治疗认知损害的苯并二氮杂环庚三烯衍生物,组合物和方法 |
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Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4342870A (en) * | 1980-03-28 | 1982-08-03 | Janssen Pharmaceutica N.V. | Novel 3-(1-piperidinylalkyl)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives |
US4804663A (en) * | 1985-03-27 | 1989-02-14 | Janssen Pharmaceutica N.V. | 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles |
-
1989
- 1989-10-16 CA CA002000786A patent/CA2000786C/en not_active Expired - Lifetime
- 1989-10-18 NZ NZ231062A patent/NZ231062A/xx unknown
- 1989-10-30 CY CY192689A patent/CY1926A/xx unknown
- 1989-10-30 EP EP89202724A patent/EP0368388B1/en not_active Expired - Lifetime
- 1989-10-30 DE DE68922577T patent/DE68922577T2/de not_active Expired - Lifetime
- 1989-10-30 AT AT89202724T patent/ATE122349T1/de active
- 1989-10-30 DE DE122007000081C patent/DE122007000081I2/de active Active
- 1989-10-30 ES ES89202724T patent/ES2075036T3/es not_active Expired - Lifetime
- 1989-11-03 IL IL92208A patent/IL92208A0/xx not_active IP Right Cessation
- 1989-11-06 FI FI895261A patent/FI92201C/fi active Protection Beyond IP Right Term
- 1989-11-06 NO NO894411A patent/NO173015C/no not_active IP Right Cessation
- 1989-11-06 AU AU44436/89A patent/AU614437B2/en not_active Expired
- 1989-11-06 IE IE356489A patent/IE66370B1/en not_active IP Right Cessation
- 1989-11-06 ZA ZA898436A patent/ZA898436B/xx unknown
- 1989-11-06 DK DK551989A patent/DK169923B1/da not_active IP Right Cessation
- 1989-11-06 PT PT92206A patent/PT92206B/pt not_active IP Right Cessation
- 1989-11-07 KR KR1019890016114A patent/KR0146053B1/ko not_active IP Right Cessation
- 1989-11-07 JP JP1289842A patent/JP2758045B2/ja not_active Expired - Lifetime
-
1996
- 1996-07-18 HK HK131696A patent/HK131696A/xx not_active IP Right Cessation
-
2004
- 2004-05-20 CL CL200401183A patent/CL43432B/es active
-
2007
- 2007-09-12 LU LU91362C patent/LU91362I2/fr unknown
- 2007-10-15 CY CY200700025C patent/CY2007025I1/el unknown
- 2007-10-17 NL NL300298C patent/NL300298I2/nl unknown
- 2007-12-21 NO NO2007017C patent/NO2007017I2/no unknown
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B1 | Patent granted (law 1993) | ||
CTFF | Application for supplementary protection certificate (spc) filed |
Spc suppl protection certif: CA 2007 00071 Filing date: 20071219 Expiry date: 20141106 |
|
CTFG | Supplementary protection certificate (spc) issued |
Free format text: PRODUCT NAME: PALIPERIDON ((PLUS MINUS)-3-{2-[4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)PIPERIDINO]ETHYL}-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ON) Spc suppl protection certif: CA 2007 00071 Filing date: 20071219 |
|
PUP | Patent expired |