CN103874487A - R(+)-n-甲酰-炔丙基-氨基茚满 - Google Patents
R(+)-n-甲酰-炔丙基-氨基茚满 Download PDFInfo
- Publication number
- CN103874487A CN103874487A CN201280049741.8A CN201280049741A CN103874487A CN 103874487 A CN103874487 A CN 103874487A CN 201280049741 A CN201280049741 A CN 201280049741A CN 103874487 A CN103874487 A CN 103874487A
- Authority
- CN
- China
- Prior art keywords
- rasagiline
- pharmaceutical composition
- formyl
- propargyl
- approximately
- 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.)
- Pending
Links
- PETXFKWYHQOVRD-CYBMUJFWSA-N C#CCN([C@H]1c2ccccc2CC1)C=O Chemical compound C#CCN([C@H]1c2ccccc2CC1)C=O PETXFKWYHQOVRD-CYBMUJFWSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C233/03—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to hydrogen atoms
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161545422P | 2011-10-10 | 2011-10-10 | |
| US61/545,422 | 2011-10-10 | ||
| PCT/US2012/059356 WO2013055687A2 (en) | 2011-10-10 | 2012-10-09 | R(+)-n-formyl-propargyl-aminoindan |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103874487A true CN103874487A (zh) | 2014-06-18 |
Family
ID=48042235
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280049741.8A Pending CN103874487A (zh) | 2011-10-10 | 2012-10-09 | R(+)-n-甲酰-炔丙基-氨基茚满 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9346746B2 (enExample) |
| EP (1) | EP2766002A4 (enExample) |
| JP (1) | JP2014534196A (enExample) |
| KR (1) | KR20140090996A (enExample) |
| CN (1) | CN103874487A (enExample) |
| AR (1) | AR088297A1 (enExample) |
| AU (1) | AU2012323349A1 (enExample) |
| BR (1) | BR112014008555A2 (enExample) |
| CA (1) | CA2851276A1 (enExample) |
| EA (1) | EA201490761A1 (enExample) |
| HK (1) | HK1200315A1 (enExample) |
| IL (1) | IL231721A0 (enExample) |
| MX (1) | MX2014004308A (enExample) |
| WO (1) | WO2013055687A2 (enExample) |
| ZA (1) | ZA201403043B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1991214B1 (en) * | 2006-02-21 | 2015-08-05 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of multiple system atrophy |
| EP2007369A4 (en) | 2006-04-03 | 2009-07-01 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF LEG SYNDROME WITHOUT REST |
| EA016820B1 (ru) * | 2006-12-14 | 2012-07-30 | Тева Фармасьютикал Индастриз, Лтд. | Кристаллическое твердое основание разагилина |
| NZ586025A (en) * | 2008-01-11 | 2012-08-31 | Teva Pharma | Rasagiline mesylate tablet coated with a composisiton comprising methacrylic acid - ethyl acrylate copolymer and triethyl citrate |
| ES2389353T3 (es) * | 2008-06-10 | 2012-10-25 | Teva Pharmaceutical Industries Ltd. | Cápsulas de gelatina blanda de rasagilina |
| RS53504B1 (sr) | 2009-07-09 | 2015-02-27 | Ratiopharm Gmbh | Soli razagilina i njihovi farmaceutski preparati |
| US20110130466A1 (en) * | 2009-10-09 | 2011-06-02 | Stefan Lorenzl | Use of rasagiline for the treatment of progressive supranuclear palsy |
| EP2939669A1 (en) * | 2009-12-22 | 2015-11-04 | Teva Pharmaceutical Industries, Ltd. | 3-keto-n-propargyl-1-aminoindan |
| AU2011282716A1 (en) | 2010-07-27 | 2013-03-14 | Teva Pharmaceutical Industries Ltd. | Dispersions of rasagiline citrate |
| AU2012323351A1 (en) | 2011-10-10 | 2014-05-22 | Teva Pharmaceutical Industries Ltd. | R(+)-N-methyl-propargyl-aminoindan |
| JP2015529196A (ja) | 2012-08-17 | 2015-10-05 | 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 | ラサギリンの非経口製剤 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997012583A2 (en) * | 1995-09-20 | 1997-04-10 | Teva Pharmaceutical Industries Ltd. | Stable compositions containing n-propargyl-1-aminoindan |
| US5877221A (en) * | 1994-01-10 | 1999-03-02 | Teva Pharmaceutical Industries, Ltd. | Compositions containing and methods of using 1-aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives |
| US6492426B1 (en) * | 1999-10-27 | 2002-12-10 | Teva Pharmaceutical Industries, Ltd. | Use of 1-aminoindan derivatives for treatment of mania in bipolar mood disorder |
| US20110152381A1 (en) * | 2009-12-22 | 2011-06-23 | Anton Frenkel | 3-keto-n-propargyl-1-aminoindan |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3201470A (en) * | 1965-08-17 | Chsx c cech | ||
| US5744500A (en) | 1990-01-03 | 1998-04-28 | Teva Pharmaceutical Industries, Ltd. | Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof |
| IL92952A (en) | 1990-01-03 | 1994-06-24 | Teva Pharma | R-enantiomers of n-propargyl-1-aminoindan compounds, their preparation and pharmaceutical compositions containing them |
| IL99759A (en) | 1991-10-16 | 1997-06-10 | Teva Pharma | Mono-fluorinated derivatives of n-propargyl-1-aminoindan, their preparation and pharmaceutical compositions containing them |
| IL111240A (en) * | 1993-10-18 | 2001-10-31 | Teva Pharma | Salts of r(+) - enantiomers of n- propargyl-1-aminoindan and pharmaceutical compositions comprising them |
| AU1867095A (en) * | 1994-01-10 | 1995-08-01 | Technion Research & Development Foundation Ltd. | 1-aminoindan derivatives and compositions thereof |
| IL118836A (en) | 1996-07-11 | 2001-01-11 | Teva Pharma | Pharmaceutical compositions comprising s-(-)-n-propargyl-1-aminoindan |
| DE69732984T2 (de) | 1996-12-18 | 2006-02-16 | Teva Pharmaceutical Industries Ltd. | Aminoindanderivate |
| EP2526944B1 (en) | 2002-11-15 | 2016-06-01 | Teva Pharmaceutical Industries Limited | Use of rasagiline with or without riluzole to treat amyotrophic lateral sclerosis |
| CA2515200C (en) | 2003-02-06 | 2013-10-08 | University Of Georgia Research Foundation, Inc. | Galacturonosyltransferases, nucleic acids encoding same and uses therefor |
| EP1778196A4 (en) | 2004-07-26 | 2008-12-17 | Teva Pharma | PHARMACEUTICAL DOSAGES CONTAINING RASAGILINE |
| CN101098685A (zh) | 2004-11-24 | 2008-01-02 | 特瓦制药工业有限公司 | 雷沙吉兰经口崩解组合物 |
| KR20140103356A (ko) | 2005-02-23 | 2014-08-26 | 테바 파마슈티컬 인더스트리즈 리미티드 | 함량 균일성이 개선된 라사길린 제형 |
| EP1954667B1 (en) | 2005-11-17 | 2017-02-08 | Teva Pharmaceutical Industries Ltd | Methods for isolating propargylated aminoindans |
| US7572834B1 (en) | 2005-12-06 | 2009-08-11 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations and processes for their preparation |
| EP1991214B1 (en) | 2006-02-21 | 2015-08-05 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of multiple system atrophy |
| EP2007369A4 (en) | 2006-04-03 | 2009-07-01 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF LEG SYNDROME WITHOUT REST |
| EP1892233A1 (de) | 2006-08-18 | 2008-02-27 | Ratiopharm GmbH | Neue Salze des Wirkstoffs Rasagilin |
| WO2008076315A1 (en) | 2006-12-14 | 2008-06-26 | Teva Pharmaceutical Industries, Ltd. | Tannate salt of rasagiline |
| EA016820B1 (ru) | 2006-12-14 | 2012-07-30 | Тева Фармасьютикал Индастриз, Лтд. | Кристаллическое твердое основание разагилина |
| EP1987816A1 (de) | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| EP2194780A4 (en) | 2007-09-05 | 2010-10-27 | Teva Pharma | METHOD FOR TREATING GLAUCOMA BY RASAGILINE |
| US8188149B2 (en) | 2007-09-17 | 2012-05-29 | Teva Pharmaceutical Industries, Ltd. | Use of R(+)-N-propargy1-1-aminoindan to treat or prevent hearing loss |
| NZ586025A (en) | 2008-01-11 | 2012-08-31 | Teva Pharma | Rasagiline mesylate tablet coated with a composisiton comprising methacrylic acid - ethyl acrylate copolymer and triethyl citrate |
| ES2389353T3 (es) | 2008-06-10 | 2012-10-25 | Teva Pharmaceutical Industries Ltd. | Cápsulas de gelatina blanda de rasagilina |
| JP2011522892A (ja) | 2008-06-13 | 2011-08-04 | 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 | パーキンソン病緩和のためのラサギリン |
| CA2727021A1 (en) | 2008-06-19 | 2009-12-23 | Teva Pharmaceutical Industries Ltd. | Process for purifying rasagiline base |
| WO2009154777A2 (en) | 2008-06-19 | 2009-12-23 | Teva Pharmaceutical Industries, Ltd. | Process for preparing and drying solid rasagiline base |
| DE102008064061A1 (de) | 2008-12-19 | 2010-06-24 | Ratiopharm Gmbh | Feste Zusammensetzung mit dem Wirkstoff Rasagilin |
| US8080584B2 (en) | 2009-01-23 | 2011-12-20 | Teva Pharmaceuticals Industries, Ltd. | Delayed release rasagiline citrate formulation |
| RS53504B1 (sr) | 2009-07-09 | 2015-02-27 | Ratiopharm Gmbh | Soli razagilina i njihovi farmaceutski preparati |
| US20110130466A1 (en) | 2009-10-09 | 2011-06-02 | Stefan Lorenzl | Use of rasagiline for the treatment of progressive supranuclear palsy |
| CN102048717B (zh) * | 2009-10-29 | 2014-02-19 | 重庆医药工业研究院有限责任公司 | 一种稳定的雷沙吉兰组合物 |
| AU2011282716A1 (en) | 2010-07-27 | 2013-03-14 | Teva Pharmaceutical Industries Ltd. | Dispersions of rasagiline citrate |
| AU2011282720B2 (en) | 2010-07-27 | 2016-12-22 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of olfactory dysfunction |
| EA201390613A1 (ru) | 2010-10-26 | 2013-11-29 | Тева Фармасьютикал Индастриз Лтд. | Обогащенный дейтерием расагилин |
| AU2012323351A1 (en) | 2011-10-10 | 2014-05-22 | Teva Pharmaceutical Industries Ltd. | R(+)-N-methyl-propargyl-aminoindan |
| US20130089611A1 (en) | 2011-10-10 | 2013-04-11 | Teva Pharmaceutical Industries, Ltd. | Rasagiline citramide |
| JP2015529196A (ja) | 2012-08-17 | 2015-10-05 | 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 | ラサギリンの非経口製剤 |
-
2012
- 2012-10-09 KR KR1020147012454A patent/KR20140090996A/ko not_active Withdrawn
- 2012-10-09 JP JP2014535789A patent/JP2014534196A/ja active Pending
- 2012-10-09 EA EA201490761A patent/EA201490761A1/ru unknown
- 2012-10-09 BR BR112014008555A patent/BR112014008555A2/pt not_active IP Right Cessation
- 2012-10-09 HK HK15100235.8A patent/HK1200315A1/xx unknown
- 2012-10-09 US US13/647,685 patent/US9346746B2/en not_active Expired - Fee Related
- 2012-10-09 CN CN201280049741.8A patent/CN103874487A/zh active Pending
- 2012-10-09 AU AU2012323349A patent/AU2012323349A1/en not_active Abandoned
- 2012-10-09 MX MX2014004308A patent/MX2014004308A/es unknown
- 2012-10-09 WO PCT/US2012/059356 patent/WO2013055687A2/en not_active Ceased
- 2012-10-09 CA CA2851276A patent/CA2851276A1/en not_active Abandoned
- 2012-10-09 EP EP12839776.7A patent/EP2766002A4/en not_active Withdrawn
- 2012-10-10 AR ARP120103781A patent/AR088297A1/es unknown
-
2014
- 2014-03-26 IL IL231721A patent/IL231721A0/en unknown
- 2014-04-25 ZA ZA2014/03043A patent/ZA201403043B/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5877221A (en) * | 1994-01-10 | 1999-03-02 | Teva Pharmaceutical Industries, Ltd. | Compositions containing and methods of using 1-aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives |
| WO1997012583A2 (en) * | 1995-09-20 | 1997-04-10 | Teva Pharmaceutical Industries Ltd. | Stable compositions containing n-propargyl-1-aminoindan |
| US6492426B1 (en) * | 1999-10-27 | 2002-12-10 | Teva Pharmaceutical Industries, Ltd. | Use of 1-aminoindan derivatives for treatment of mania in bipolar mood disorder |
| US20110152381A1 (en) * | 2009-12-22 | 2011-06-23 | Anton Frenkel | 3-keto-n-propargyl-1-aminoindan |
Non-Patent Citations (2)
| Title |
|---|
| TARA SINGH等: "Antimalarials. 7-Chloro-4-(substituted amino)quinolines", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 14, no. 4, 31 December 1971 (1971-12-31), XP002337637, DOI: 10.1021/jm00286a003 * |
| 张青山: "《有机合成反应基础》", 31 December 2004, 高等教育出版社, article "用羧酸的N-酰化" * |
Also Published As
| Publication number | Publication date |
|---|---|
| US9346746B2 (en) | 2016-05-24 |
| ZA201403043B (en) | 2015-08-26 |
| AR088297A1 (es) | 2014-05-21 |
| IL231721A0 (en) | 2014-05-28 |
| KR20140090996A (ko) | 2014-07-18 |
| NZ624206A (en) | 2016-11-25 |
| HK1200315A1 (en) | 2015-08-07 |
| MX2014004308A (es) | 2014-07-24 |
| WO2013055687A3 (en) | 2013-07-25 |
| EA201490761A1 (ru) | 2014-11-28 |
| JP2014534196A (ja) | 2014-12-18 |
| CA2851276A1 (en) | 2013-04-18 |
| EP2766002A4 (en) | 2015-07-01 |
| WO2013055687A2 (en) | 2013-04-18 |
| EP2766002A2 (en) | 2014-08-20 |
| US20130089612A1 (en) | 2013-04-11 |
| BR112014008555A2 (pt) | 2017-04-18 |
| AU2012323349A1 (en) | 2014-05-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20140618 |
|
| RJ01 | Rejection of invention patent application after publication |