EA200101179A1 - Полиморфные модификации кристаллического (2-бензгидрил-1-азабицикло[2.2.2]окт-3-ил)-(5-изопропил-2-метоксибензил)-аммония хлорида в качестве антагонистов рецептора нейрокинина 1 (nk-1) - Google Patents
Полиморфные модификации кристаллического (2-бензгидрил-1-азабицикло[2.2.2]окт-3-ил)-(5-изопропил-2-метоксибензил)-аммония хлорида в качестве антагонистов рецептора нейрокинина 1 (nk-1)Info
- Publication number
- EA200101179A1 EA200101179A1 EA200101179A EA200101179A EA200101179A1 EA 200101179 A1 EA200101179 A1 EA 200101179A1 EA 200101179 A EA200101179 A EA 200101179A EA 200101179 A EA200101179 A EA 200101179A EA 200101179 A1 EA200101179 A1 EA 200101179A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- benzhydryl
- azabicyclo
- methoxybenzyl
- isopropyl
- crystalline
- Prior art date
Links
- 101000831616 Homo sapiens Protachykinin-1 Proteins 0.000 title 2
- 102100024304 Protachykinin-1 Human genes 0.000 title 2
- ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 title 2
- AXFGBGHZCXQFRG-UHFFFAOYSA-N 2-benzhydryl-n-[(2-methoxy-5-propan-2-ylphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine;hydrochloride Chemical compound Cl.COC1=CC=C(C(C)C)C=C1CNC1C(C(C=2C=CC=CC=2)C=2C=CC=CC=2)N2CCC1CC2 AXFGBGHZCXQFRG-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- -1 2-benzhydryl-1-azabicyclo [2.2.2] octyl-3-yl Chemical group 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 239000002775 capsule Substances 0.000 abstract 1
- 238000002512 chemotherapy Methods 0.000 abstract 1
- CKQQMPJQZXIYMJ-UHFFFAOYSA-N dihydrate;dihydrochloride Chemical compound O.O.Cl.Cl CKQQMPJQZXIYMJ-UHFFFAOYSA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000012986 modification Methods 0.000 abstract 1
- 230000004048 modification Effects 0.000 abstract 1
- 230000008673 vomiting Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
- C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (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)
- Veterinary Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Две кристаллические полиморфные формы дигидрата дигидрохлорида (2-бензгидрил-1-азабицикло[2.2.2]октил-3-ил)-(5-изопропил-2-метоксибензил)-амина представляют собой форму I и форму II. Фармацевтическая композиция, содержащая, по меньшей мере, одну из этих полиморфных модификаций, имеет выгодную стабильность для приготовления препарата для лечения рвоты у пациентов, получающих химиотерапию. Введение этой фармацевтической композиции обычно пероральное, предпочтительно с помощью таблетки или капсулы, либо внутривенное. Также раскрыт способ получения форм I и II.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14023399P | 1999-06-22 | 1999-06-22 | |
| PCT/IB2000/000756 WO2000078759A1 (en) | 1999-06-22 | 2000-06-06 | Polymorphs of crystalline (2-benzhydryl-1-azabicyclo[2,2,2]oct-3-yl)-(5-isopropyl-2-methoxybenzyl)-ammoniumchloride as nk-1 receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200101179A1 true EA200101179A1 (ru) | 2002-06-27 |
| EA004264B1 EA004264B1 (ru) | 2004-02-26 |
Family
ID=22490317
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200101179A EA004264B1 (ru) | 1999-06-22 | 2000-06-06 | Полиморфные модификации кристаллического (2-бензгидрил-1-азабицикло[2.2.2]окт-3-ил)-(5-изопропил-2-метоксибензил)аммония хлорида в качестве антагонистов рецептора нейрокинина 1 (nk-1) |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US6262067B1 (ru) |
| EP (1) | EP1187834A1 (ru) |
| JP (1) | JP2003502425A (ru) |
| KR (1) | KR20020030280A (ru) |
| CN (1) | CN1390216A (ru) |
| AP (1) | AP2001002367A0 (ru) |
| AR (1) | AR024411A1 (ru) |
| AU (1) | AU767336B2 (ru) |
| BG (1) | BG106205A (ru) |
| BR (1) | BR0011835A (ru) |
| CA (1) | CA2375265A1 (ru) |
| CO (1) | CO5190663A1 (ru) |
| CZ (1) | CZ20014458A3 (ru) |
| DZ (1) | DZ3055A1 (ru) |
| EA (1) | EA004264B1 (ru) |
| EC (1) | ECSP003538A (ru) |
| EE (1) | EE200100698A (ru) |
| HR (1) | HRP20010920A2 (ru) |
| HU (1) | HUP0201694A3 (ru) |
| IL (1) | IL146410A0 (ru) |
| IS (1) | IS6161A (ru) |
| MA (1) | MA26744A1 (ru) |
| MX (1) | MXPA02000033A (ru) |
| NO (1) | NO20016187D0 (ru) |
| NZ (1) | NZ515348A (ru) |
| OA (1) | OA11952A (ru) |
| PA (1) | PA8496701A1 (ru) |
| PE (1) | PE20010322A1 (ru) |
| PL (1) | PL352899A1 (ru) |
| SK (1) | SK18672001A3 (ru) |
| TN (1) | TNSN00137A1 (ru) |
| TR (1) | TR200103688T2 (ru) |
| UY (1) | UY26211A1 (ru) |
| WO (1) | WO2000078759A1 (ru) |
| ZA (1) | ZA200110387B (ru) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6387925B1 (en) * | 1999-06-01 | 2002-05-14 | Pfizer Inc. | Polymorphs of a crystalline azo-bicyclo (2.2.2) oct-3-yl amine citrate and their pharmaceutical compositions |
| US6756379B2 (en) | 2001-07-26 | 2004-06-29 | Taro Pharmaceutical Industries Ltd. | Non-sedating barbiturate compounds as neuroprotective agents |
| US7683071B2 (en) * | 2000-07-26 | 2010-03-23 | Taro Pharmaceuticals Industries Ltd. | Composition and method for improved bioavailability and enhanced brain delivery of 5,5-diphenyl barbituric acid |
| US6939873B2 (en) * | 2000-07-26 | 2005-09-06 | Taro Pharmaceuticals Industries Limited | Non-sedating barbituric acid derivatives |
| EP1551846A1 (en) * | 2002-10-04 | 2005-07-13 | Merck Sharp & Dohme Ltd. | Azabicyclic spiroether derivatives as receptor antagonists |
| WO2004052350A2 (en) * | 2002-12-11 | 2004-06-24 | Taro Pharmaceutical Industries Limited | Method of treating movement disorders using barbituric acid derivatives |
| WO2006003651A2 (en) * | 2004-07-02 | 2006-01-12 | Taro Pharmaceutical Industries, Ltd | A process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid |
| EP2081576A4 (en) * | 2006-11-14 | 2010-06-30 | Taro Pharmaceuticals North Ame | METHOD FOR IMPROVING BIOAVAILABILITY FOR NON-EDMING BARBITURATES |
| UA102128C2 (en) * | 2008-12-05 | 2013-06-10 | Х. Луннбек А/С | Nalmefene hydrochloride dihydrate |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1990005525A1 (en) * | 1988-11-23 | 1990-05-31 | Pfizer Inc. | Quinuclidine derivatives as substance p antagonists |
| CZ281403B6 (cs) * | 1991-05-31 | 1996-09-11 | Pfizer Inc. | Chinuklidinové deriváty, způsob jejich přípravy a použití. |
| DK0668863T3 (da) * | 1992-11-12 | 1997-06-30 | Pfizer | Quinuclidinderivat som substans P-antagonist |
| US5393762A (en) * | 1993-06-04 | 1995-02-28 | Pfizer Inc. | Pharmaceutical agents for treatment of emesis |
-
2000
- 2000-05-04 US US09/564,528 patent/US6262067B1/en not_active Expired - Fee Related
- 2000-06-06 CN CN00809305A patent/CN1390216A/zh active Pending
- 2000-06-06 CA CA002375265A patent/CA2375265A1/en not_active Abandoned
- 2000-06-06 TR TR2001/03688T patent/TR200103688T2/xx unknown
- 2000-06-06 WO PCT/IB2000/000756 patent/WO2000078759A1/en not_active Application Discontinuation
- 2000-06-06 EA EA200101179A patent/EA004264B1/ru not_active IP Right Cessation
- 2000-06-06 PL PL00352899A patent/PL352899A1/xx not_active Application Discontinuation
- 2000-06-06 OA OA1200100314A patent/OA11952A/en unknown
- 2000-06-06 SK SK1867-2001A patent/SK18672001A3/sk unknown
- 2000-06-06 MX MXPA02000033A patent/MXPA02000033A/es unknown
- 2000-06-06 HU HU0201694A patent/HUP0201694A3/hu unknown
- 2000-06-06 KR KR1020017016407A patent/KR20020030280A/ko not_active Application Discontinuation
- 2000-06-06 AU AU47745/00A patent/AU767336B2/en not_active Ceased
- 2000-06-06 EP EP00929745A patent/EP1187834A1/en not_active Withdrawn
- 2000-06-06 PA PA20008496701A patent/PA8496701A1/es unknown
- 2000-06-06 AP APAP/P/2001/002367A patent/AP2001002367A0/en unknown
- 2000-06-06 IL IL14641000A patent/IL146410A0/xx unknown
- 2000-06-06 NZ NZ515348A patent/NZ515348A/en unknown
- 2000-06-06 BR BR0011835-4A patent/BR0011835A/pt not_active IP Right Cessation
- 2000-06-06 JP JP2001504925A patent/JP2003502425A/ja active Pending
- 2000-06-06 CZ CZ20014458A patent/CZ20014458A3/cs unknown
- 2000-06-06 EE EEP200100698A patent/EE200100698A/xx unknown
- 2000-06-13 CO CO00043885A patent/CO5190663A1/es not_active Application Discontinuation
- 2000-06-20 PE PE2000000613A patent/PE20010322A1/es not_active Application Discontinuation
- 2000-06-20 AR ARP000103053A patent/AR024411A1/es not_active Application Discontinuation
- 2000-06-20 UY UY26211A patent/UY26211A1/es not_active Application Discontinuation
- 2000-06-21 TN TNTNSN00137A patent/TNSN00137A1/fr unknown
- 2000-06-21 MA MA26007A patent/MA26744A1/fr unknown
- 2000-06-21 DZ DZ000113A patent/DZ3055A1/xx active
- 2000-06-22 EC EC2000003538A patent/ECSP003538A/es unknown
-
2001
- 2001-11-13 IS IS6161A patent/IS6161A/is unknown
- 2001-12-10 BG BG106205A patent/BG106205A/bg unknown
- 2001-12-11 HR HR20010920A patent/HRP20010920A2/hr not_active Application Discontinuation
- 2001-12-18 NO NO20016187A patent/NO20016187D0/no not_active Application Discontinuation
- 2001-12-19 ZA ZA200110387A patent/ZA200110387B/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2078578A1 (en) | Medical use for tachykinin antagonists | |
| MY138086A (en) | Novel urea derivative as vanilloid receptor-1 antagonist | |
| CY1106802T1 (el) | Ανασταλτικη της εκκρισης γαστρικου οξεος συνθεση | |
| AU2001293233A1 (en) | Aza heterocyclic derivatives and their therapeutic use | |
| ATE519486T1 (de) | Pharmazeutische zusammensetzung mit einem monoamin-neurotransmitter-wiederaufnahmehemmer und einem acetylcholinesterase-hemmer | |
| CA2432578A1 (en) | Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists | |
| DK0734383T3 (da) | Cykliske amidderivater som neurokinin-A-antagonister | |
| WO2001027111A3 (de) | Bicyclische imidazo-3-yl-aminderivate | |
| UA85359C2 (ru) | Таблетка, содержащая гранулированный материал с kmd-3213 | |
| WO2003053945A3 (en) | Urea derivatives and their use as vanilloid receptor antagonists | |
| EA200101179A1 (ru) | Полиморфные модификации кристаллического (2-бензгидрил-1-азабицикло[2.2.2]окт-3-ил)-(5-изопропил-2-метоксибензил)-аммония хлорида в качестве антагонистов рецептора нейрокинина 1 (nk-1) | |
| ATE352543T1 (de) | Ein dioxino(2,3-g)chinolin-9-carbonsäure derivat als nk3 rezeptor antagonist | |
| ATE151637T1 (de) | Heterozyklische verbindungen | |
| WO2001027110A3 (de) | Am sechsring substituierte, bicyclische imidazo-3-yl-aminderivate | |
| ATE268174T1 (de) | Sibutramin und orlistat enthaltende pharmazeutische zusammensetzungen | |
| NO20031410L (no) | Anvendelse av distamycinderivater for fremstilling av medikamenter | |
| EA200100982A1 (ru) | Полиморфные модификации кристаллического цитрата (2-бензгидрил-1-азабицикло[2.2.2]окт-3-ил)-(5-изопропил-2-метоксибензил)-амина в качестве антагонистов рецепторов нейрокинина 1 (nk1) | |
| TW200517127A (en) | Novel composition | |
| BG106180A (en) | Pharmaceutical composition containing sibutramine and orlistat | |
| ES2197781A1 (es) | Composiciones farmaceuticas liquidas de base acuosa en forma de suspension para la administracion por via oral de ibuprofeno. | |
| EA200101108A1 (ru) | Полиморфные модификации кристаллического цитрата азабицикло[2.2.2]октан-3-амина и их фармацевтические композиции | |
| KR940701407A (ko) | 레닌 억제제로서의 하이드록시아지도 유도체 및 관련 화합물 | |
| AR036131A1 (es) | Derivados de benzo (g) quinolina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la fabricacion de un medicamento | |
| ES8707729A1 (es) | Un procedimiento para la preparacion de hexahidroarilquinolizinas sustituidas. | |
| EP1172106A3 (en) | Use of fluoroalkoxybenzylamino derivatives of nitrogen containing heterocycles as substance P receptor antagonists |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |