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)
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2007217349B9 (en) * | 2006-02-21 | 2013-06-27 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of Multiple System Atrophy |
| CA2646250A1 (en) | 2006-04-03 | 2007-10-18 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of restless legs syndrome |
| PT2101569E (pt) * | 2006-12-14 | 2012-01-13 | Teva Pharma | Base de rasagilina sólida cristalina |
| KR20100107028A (ko) * | 2008-01-11 | 2010-10-04 | 테바 파마슈티컬 인더스트리즈 리미티드 | 라사길린 제형, 그들의 제법 및 용도 |
| EP2285214B1 (en) * | 2008-06-10 | 2012-05-16 | Teva Pharmaceutical Industries Ltd. | Rasagiline soft gelatin capsules |
| PL2451771T3 (pl) | 2009-07-09 | 2014-12-31 | Ratiopharm Gmbh | Sole rasagiliny i ich preparaty farmaceutyczne |
| WO2011042812A1 (en) * | 2009-10-09 | 2011-04-14 | Stefan Lorenzl | Use of rasagiline for the treatment of progressive supranuclear palsy |
| MX2012007375A (es) * | 2009-12-22 | 2012-07-30 | Teva Pharma | 3-ceto-n-propargil 1-aminoindano. |
| JP2013537530A (ja) | 2010-07-27 | 2013-10-03 | 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 | ラサギリンシトレートの分散物 |
| AU2012323351A1 (en) | 2011-10-10 | 2014-05-22 | Teva Pharmaceutical Industries Ltd. | R(+)-N-methyl-propargyl-aminoindan |
| WO2014028868A1 (en) | 2012-08-17 | 2014-02-20 | Teva Pharmaceutical Industries Ltd. | Parenteral formulation of rasagiline |
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 | ||
| 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 |
| 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 |
| 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 |
| ATE346598T1 (de) * | 1994-01-10 | 2006-12-15 | Teva Pharma | 1-aminoindanderivate und zusammensetzungen hiervon |
| IL118836A (en) | 1996-07-11 | 2001-01-11 | Teva Pharma | Pharmaceutical compositions comprising s-(-)-n-propargyl-1-aminoindan |
| DK0966435T3 (da) | 1996-12-18 | 2005-08-15 | Teva Pharma | Aminoindanderivater |
| EP1567152B1 (en) | 2002-11-15 | 2013-08-14 | Teva Pharmaceutical Industries Limited | Use of rasagiline with riluzole to treat amyotrophic lateral sclerosis |
| US7619077B2 (en) | 2003-02-06 | 2009-11-17 | University Of Georgia Research Foundation | Nucleic acids encoding a galacturonosyl tranferase enzyme (GALAT1) from arabidopsis |
| EP1778196A4 (en) | 2004-07-26 | 2008-12-17 | Teva Pharma | PHARMACEUTICAL DOSAGES CONTAINING RASAGILINE |
| US20090111892A1 (en) | 2004-11-24 | 2009-04-30 | Shulamit Patashnik | Rasagiline Orally Disintegrating Compositions |
| US7815942B2 (en) | 2005-02-23 | 2010-10-19 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations of improved content uniformity |
| US7491847B2 (en) | 2005-11-17 | 2009-02-17 | 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 |
| AU2007217349B9 (en) | 2006-02-21 | 2013-06-27 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of Multiple System Atrophy |
| CA2646250A1 (en) | 2006-04-03 | 2007-10-18 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of restless legs syndrome |
| EP1892233A1 (de) | 2006-08-18 | 2008-02-27 | Ratiopharm GmbH | Neue Salze des Wirkstoffs Rasagilin |
| PT2101569E (pt) | 2006-12-14 | 2012-01-13 | Teva Pharma | Base de rasagilina sólida cristalina |
| EA016843B1 (ru) | 2006-12-14 | 2012-07-30 | Тева Фармасьютикал Индастриз, Лтд. | Таннат разагилина |
| EP1987816A1 (de) | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| US20090062400A1 (en) | 2007-09-05 | 2009-03-05 | Laurence Oron | Method of treating glaucoma using 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 |
| KR20100107028A (ko) | 2008-01-11 | 2010-10-04 | 테바 파마슈티컬 인더스트리즈 리미티드 | 라사길린 제형, 그들의 제법 및 용도 |
| EP2285214B1 (en) | 2008-06-10 | 2012-05-16 | Teva Pharmaceutical Industries Ltd. | Rasagiline soft gelatin capsules |
| BRPI0909894A2 (pt) | 2008-06-13 | 2015-07-28 | Teva Pharma | "método de redução da velocidade de progressão de mal de parkinson em um paciente com mal de parkinson em estágio inicial, método de redução da velocidade de progressão de mal de parkinson, método de atraso da necessidade de terapia antiparkinsoniana sintomática em um paciente de mal de parkinson em estágio inicial, método de redução do risco de um paciente com mal de parkinson que necessita de terapia antiparkinsoniana, método de redução do declínio funcional de um paciente com mal de parkinson em estágio inicial, método de redução do declínio funcional em um paciente com mal de parkinson, método de tratamento de um paciente que exibe sinais iniciais de mal de parkinson, método de redução da fadiga em um paciente com mal de parkinson em estágio inicial, método de redução da velocidade de progressão clínica e tratamento de sintomas de mal de parkinson em um paciente com mal de parkinson, rasagilina ou um sal farmaceuticamente aceitável de rasagilina, composição farmacêutica. |
| US7968749B2 (en) | 2008-06-19 | 2011-06-28 | Teva Pharmaceutical Industries, Ltd. | Process for preparing and drying solid rasagiline base |
| AU2009260733B2 (en) | 2008-06-19 | 2015-01-29 | Teva Pharmaceutical Industries, Ltd. | Process for purifying rasagiline base |
| DE102008064061A1 (de) | 2008-12-19 | 2010-06-24 | Ratiopharm Gmbh | Feste Zusammensetzung mit dem Wirkstoff Rasagilin |
| US20100189791A1 (en) | 2009-01-23 | 2010-07-29 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline malate formulation |
| PL2451771T3 (pl) | 2009-07-09 | 2014-12-31 | Ratiopharm Gmbh | Sole rasagiliny i ich preparaty farmaceutyczne |
| WO2011042812A1 (en) | 2009-10-09 | 2011-04-14 | 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 |
| EP2603212A4 (en) | 2010-07-27 | 2014-01-08 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF SMOKING DISORDER |
| JP2013537530A (ja) | 2010-07-27 | 2013-10-03 | 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 | ラサギリンシトレートの分散物 |
| BR112013010308A2 (pt) | 2010-10-26 | 2016-07-05 | Teva Pharma | rasagilina de deutério enriquecido |
| 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 |
| WO2014028868A1 (en) | 2012-08-17 | 2014-02-20 | Teva Pharmaceutical Industries Ltd. | Parenteral formulation of rasagiline |
-
2012
- 2012-10-09 BR BR112014008555A patent/BR112014008555A2/pt not_active IP Right Cessation
- 2012-10-09 JP JP2014535789A patent/JP2014534196A/ja active Pending
- 2012-10-09 MX MX2014004308A patent/MX2014004308A/es unknown
- 2012-10-09 CA CA2851276A patent/CA2851276A1/en not_active Abandoned
- 2012-10-09 EP EP12839776.7A patent/EP2766002A4/en not_active Withdrawn
- 2012-10-09 EA EA201490761A patent/EA201490761A1/ru unknown
- 2012-10-09 AU AU2012323349A patent/AU2012323349A1/en not_active Abandoned
- 2012-10-09 KR KR1020147012454A patent/KR20140090996A/ko not_active Withdrawn
- 2012-10-09 CN CN201280049741.8A patent/CN103874487A/zh active Pending
- 2012-10-09 WO PCT/US2012/059356 patent/WO2013055687A2/en not_active Ceased
- 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
- 2012-10-10 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 |
|---|---|
| KR20140090996A (ko) | 2014-07-18 |
| WO2013055687A2 (en) | 2013-04-18 |
| ZA201403043B (en) | 2015-08-26 |
| BR112014008555A2 (pt) | 2017-04-18 |
| EP2766002A4 (en) | 2015-07-01 |
| HK1200315A1 (en) | 2015-08-07 |
| IL231721A0 (en) | 2014-05-28 |
| AU2012323349A1 (en) | 2014-05-22 |
| AR088297A1 (es) | 2014-05-21 |
| MX2014004308A (es) | 2014-07-24 |
| US20130089612A1 (en) | 2013-04-11 |
| EA201490761A1 (ru) | 2014-11-28 |
| NZ624206A (en) | 2016-11-25 |
| CA2851276A1 (en) | 2013-04-18 |
| US9346746B2 (en) | 2016-05-24 |
| WO2013055687A3 (en) | 2013-07-25 |
| JP2014534196A (ja) | 2014-12-18 |
| EP2766002A2 (en) | 2014-08-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103874487A (zh) | R(+)-n-甲酰-炔丙基-氨基茚满 | |
| CN103930100A (zh) | R(+)-n-甲基-炔丙基-氨基茚满 | |
| CN103857389A (zh) | 雷沙吉兰柠檬酰胺 | |
| ES2370980T3 (es) | Formulación de resagilina de liberación retardada. | |
| US12465570B2 (en) | Methods | |
| US8691872B2 (en) | Dispersions of rasagiline citrate | |
| MX2013000332A (es) | 5-cloro-4-hidroxi-1-metil-2-oxo-n-fenil-1,2-dihidroquinolina-3-ca rboxamida, sales y usos de la misma. | |
| AU2009275665A1 (en) | Polymorphic form of rasagiline mesylate | |
| CN104395291B (zh) | N‑乙基‑4‑羟基‑1‑甲基‑5‑(甲基(2,3,4,5,6‑五羟基己基)氨基)‑2‑氧代‑n‑苯基‑1,2‑二氢喹啉‑3‑甲酰胺 | |
| EP2874628B1 (en) | Salts and hydrates of antipsychotics | |
| WO2008066729A2 (en) | Boronic acid containing compositions | |
| NZ624206B2 (en) | R(+)-n-formyl-propargyl-aminoindan | |
| CN1305491A (zh) | 晶体形式的1S-[1a(2S ,3R ),9a]-6,10-二氧代-N-(2-乙氧基-5-氧代-四氢-3-呋喃基)-9[[1-异喹啉基羰基)氨基],八氢-6H-哒嗪并[1,2-A][1,2]二氮杂䓬-1-甲酰胺 |
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 |