EA200100982A1 - 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) - Google Patents
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)Info
- Publication number
- EA200100982A1 EA200100982A1 EA200100982A EA200100982A EA200100982A1 EA 200100982 A1 EA200100982 A1 EA 200100982A1 EA 200100982 A EA200100982 A EA 200100982A EA 200100982 A EA200100982 A EA 200100982A EA 200100982 A1 EA200100982 A1 EA 200100982A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- benzhydryl
- azabicyclo
- methoxybenzyl
- oct
- isopropyl
- 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
- BIUZWZLMPAUPFK-UHFFFAOYSA-N 2-benzhydryl-n-[(2-methoxy-5-propan-2-ylphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.COC1=CC=C(C(C)C)C=C1CNC1C(C(C=2C=CC=CC=2)C=2C=CC=CC=2)N2CCC1CC2 BIUZWZLMPAUPFK-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 239000002775 capsule Substances 0.000 abstract 1
- 238000002512 chemotherapy Methods 0.000 abstract 1
- -1 citrate monohydrate (2-benzhydryl-1-azabicyclo [2.2.2] oct-3-yl) - (5-isopropyl-2-methoxybenzyl) -amine Chemical compound 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
- 150000004682 monohydrates Chemical class 0.000 abstract 1
- 230000008673 vomiting Effects 0.000 abstract 1
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Двумя кристаллическими полиморфными формами моногидрата цитрата (2-бензгидрил-1-азабицикло[2.2.2]окт-3-ил)-(5-изопропил-2-метоксибензил)-амина (моногидратами) являются форма А и форма Б. Фармацевтическая композиция, содержащая, по меньшей мере, одну из этих полиморфных модификаций, обладает полезной стабильностью для приготовления препаратов для лечения острой рвоты у пациентов, получающих химиотерапию. Введение этой фармацевтической композиции осуществляется обычно перорально предпочтительно в виде таблетки или капсулы и внутривенно. Также раскрыт способ получения форм А и Б.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13699599P | 1999-06-01 | 1999-06-01 | |
PCT/IB2000/000663 WO2000073303A1 (en) | 1999-06-01 | 2000-05-17 | Polymorphs of crystalline (2-benzhydryl-1-azabicyclo[2.2.2]oct-3-yl)-(5-isopropyl-2-methoxybenzyl)-amine citrate as nk-1 receptor antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200100982A1 true EA200100982A1 (ru) | 2002-06-27 |
EA004206B1 EA004206B1 (ru) | 2004-02-26 |
Family
ID=22475353
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200100982A EA004206B1 (ru) | 1999-06-01 | 2000-05-17 | 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) |
Country Status (38)
Country | Link |
---|---|
US (1) | US6387925B1 (ru) |
EP (1) | EP1181289A1 (ru) |
JP (1) | JP2003501353A (ru) |
KR (1) | KR20020005055A (ru) |
CN (1) | CN1353712A (ru) |
AP (1) | AP2001002350A0 (ru) |
AR (1) | AR029753A1 (ru) |
AU (1) | AU767331B2 (ru) |
BG (1) | BG106139A (ru) |
BR (1) | BR0011125A (ru) |
CA (1) | CA2372236A1 (ru) |
CO (1) | CO5170468A1 (ru) |
CR (1) | CR6513A (ru) |
CZ (1) | CZ20014270A3 (ru) |
DZ (1) | DZ3051A1 (ru) |
EA (1) | EA004206B1 (ru) |
EE (1) | EE200100655A (ru) |
GT (1) | GT200000086A (ru) |
HK (1) | HK1046407A1 (ru) |
HN (1) | HN2000000076A (ru) |
HR (1) | HRP20010884A2 (ru) |
HU (1) | HUP0201798A3 (ru) |
IL (1) | IL145952A0 (ru) |
IS (1) | IS6129A (ru) |
MX (1) | MXPA01012328A (ru) |
NO (1) | NO20015845L (ru) |
NZ (1) | NZ514762A (ru) |
OA (1) | OA11955A (ru) |
PA (1) | PA8496001A1 (ru) |
PE (1) | PE20010155A1 (ru) |
PL (1) | PL352715A1 (ru) |
SK (1) | SK17342001A3 (ru) |
SV (1) | SV2002000092A (ru) |
TN (1) | TNSN00119A1 (ru) |
TR (1) | TR200103472T2 (ru) |
UY (1) | UY26177A1 (ru) |
WO (1) | WO2000073303A1 (ru) |
ZA (1) | ZA200109839B (ru) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2006503859A (ja) * | 2002-10-04 | 2006-02-02 | メルク シャープ エンド ドーム リミテッド | 受容体拮抗薬としてのアザ二環式スピロエーテル誘導体 |
JP2007524619A (ja) * | 2003-06-18 | 2007-08-30 | 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 | フルバスタチンナトリウム結晶型、その調製方法、これを含有する組成物、およびその使用法 |
US7371906B2 (en) | 2004-08-24 | 2008-05-13 | Eastman Kodak Company | Process for photo-oxidative stability improvements |
US9446029B2 (en) | 2010-07-27 | 2016-09-20 | Colorado State University Research Foundation | Use of NK-1 receptor antagonists in management of visceral pain |
CN110577522B (zh) * | 2018-06-07 | 2022-12-27 | 东莞市东阳光动物保健药品有限公司 | 马罗匹坦柠檬酸盐新晶型及其制备方法 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX18467A (es) * | 1988-11-23 | 1993-07-01 | Pfizer | Agentes terapeuticos de quinuclidinas |
WO1992021677A1 (en) * | 1991-05-31 | 1992-12-10 | Pfizer Inc. | bibNUCLIDINE DERIVATIVES |
EP0668863B1 (en) * | 1992-11-12 | 1997-01-08 | Pfizer Inc. | Quinuclidine derivative as substance p antagonist |
US5393762A (en) * | 1993-06-04 | 1995-02-28 | Pfizer Inc. | Pharmaceutical agents for treatment of emesis |
US6262067B1 (en) * | 1999-06-22 | 2001-07-17 | Pfizer Inc. | Polymorphs of a crystalline azo-bicyclo 2,2,2 OCT-3-yl amine dihydrochloride and their pharmaceutical compositions |
-
2000
- 2000-05-12 US US09/887,682 patent/US6387925B1/en not_active Expired - Fee Related
- 2000-05-17 BR BR0011125-2A patent/BR0011125A/pt not_active IP Right Cessation
- 2000-05-17 HU HU0201798A patent/HUP0201798A3/hu unknown
- 2000-05-17 EA EA200100982A patent/EA004206B1/ru not_active IP Right Cessation
- 2000-05-17 HN HN2000000076A patent/HN2000000076A/es unknown
- 2000-05-17 AU AU44246/00A patent/AU767331B2/en not_active Ceased
- 2000-05-17 PL PL00352715A patent/PL352715A1/xx not_active Application Discontinuation
- 2000-05-17 CZ CZ20014270A patent/CZ20014270A3/cs unknown
- 2000-05-17 MX MXPA01012328A patent/MXPA01012328A/es not_active Application Discontinuation
- 2000-05-17 EP EP00925526A patent/EP1181289A1/en not_active Withdrawn
- 2000-05-17 IL IL14595200A patent/IL145952A0/xx unknown
- 2000-05-17 JP JP2001500628A patent/JP2003501353A/ja active Pending
- 2000-05-17 NZ NZ514762A patent/NZ514762A/xx unknown
- 2000-05-17 TR TR2001/03472T patent/TR200103472T2/xx unknown
- 2000-05-17 SK SK1734-2001A patent/SK17342001A3/sk unknown
- 2000-05-17 EE EEP200100655A patent/EE200100655A/xx unknown
- 2000-05-17 CA CA002372236A patent/CA2372236A1/en not_active Abandoned
- 2000-05-17 CN CN00808340A patent/CN1353712A/zh active Pending
- 2000-05-17 WO PCT/IB2000/000663 patent/WO2000073303A1/en not_active Application Discontinuation
- 2000-05-17 AP APAP/P/2001/002350A patent/AP2001002350A0/en unknown
- 2000-05-17 OA OA1200100317A patent/OA11955A/en unknown
- 2000-05-17 KR KR1020017015324A patent/KR20020005055A/ko not_active Application Discontinuation
- 2000-05-19 PA PA20008496001A patent/PA8496001A1/es unknown
- 2000-05-26 CO CO00039192A patent/CO5170468A1/es not_active Application Discontinuation
- 2000-05-29 UY UY26177A patent/UY26177A1/es not_active Application Discontinuation
- 2000-05-30 PE PE2000000517A patent/PE20010155A1/es not_active Application Discontinuation
- 2000-05-30 AR ARP000102664A patent/AR029753A1/es unknown
- 2000-05-30 GT GT200000086A patent/GT200000086A/es unknown
- 2000-05-31 DZ DZ000102A patent/DZ3051A1/xx active
- 2000-05-31 SV SV2000000092A patent/SV2002000092A/es unknown
- 2000-05-31 TN TNTNSN00119A patent/TNSN00119A1/fr unknown
-
2001
- 2001-10-26 IS IS6129A patent/IS6129A/is unknown
- 2001-11-23 BG BG106139A patent/BG106139A/bg unknown
- 2001-11-27 CR CR6513A patent/CR6513A/es not_active Application Discontinuation
- 2001-11-27 HR HR20010884A patent/HRP20010884A2/hr not_active Application Discontinuation
- 2001-11-29 ZA ZA200109839A patent/ZA200109839B/xx unknown
- 2001-11-30 NO NO20015845A patent/NO20015845L/no not_active Application Discontinuation
-
2002
- 2002-10-30 HK HK02107840.5A patent/HK1046407A1/zh unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EP0498069B1 (en) | New use of peptide derivative | |
US6262081B1 (en) | Composition for and method of treating neurological disorders | |
BRPI0610187B1 (pt) | Tablete dispersável ou um solvato ou sal farmaceuticamente aceitável do mesmo, e excipientes farmaceuticamente aceitáveis, processo para a preparação dos mesmos, e uso de composto ou de um sal ou solvato farmaceuticamente aceitável do mesmo | |
MY129234A (en) | Oral pharmaceutical forms of administration with a delayed action with tramadol. | |
IL149496A (en) | Pharmaceutical compositions and their use in the treatment of the gastrointestinal tract | |
EA200200651A1 (ru) | Замещенные пиперидины, содержащие эти соединения лекарственные средства и способ их получения | |
UA85359C2 (ru) | Таблетка, содержащая гранулированный материал с kmd-3213 | |
US4694010A (en) | Anticonvulsant compositions and method | |
RU93004793A (ru) | Производные хиназолина, способ их получения, фармацевтическая композиция на их основе | |
RU93004860A (ru) | Гетероциклические соединения, способ их получения, использование и фармацевтическая композиция | |
HU226976B1 (en) | Use of pirrolidine derivatives having kappa-opium-agonist effect for the preparation of a medicament for treating of inflammatory diseases of the intestine | |
ES8505379A1 (es) | Un metodo de fabricar 1, 4-dihidropiridina-3-carboxilatos | |
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) | |
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) | |
TR200101163T2 (tr) | Safra suyu ikameli fenil-alkenoilguanidinler, üretim yöntemleri, kullanımları | |
JP2008509974A (ja) | 抗炎症剤 | |
EA200300247A1 (ru) | Фармацевтическая композиция, содержащая циталопрам | |
EP0393696A2 (en) | 7-(Substituted)amino)-8-(substituted)Carbonyl)-methylamino-1-oxaspiro (4,5)decanes as diuretics antiinflammatory, and cerebrovascular agents | |
KR920010388B1 (ko) | 9,10-디하이드로 에르고트 알카로이드를 함유하는 서방성 약학제제의 제조방법 | |
EA200101108A1 (ru) | Полиморфные модификации кристаллического цитрата азабицикло[2.2.2]октан-3-амина и их фармацевтические композиции | |
KR20050121236A (ko) | 치매 환자에서 초조 증상을 치료하기 위한 카르바마제핀유도체의 용도 | |
JP3064027B2 (ja) | 血管新生阻害剤 | |
GB9420748D0 (en) | 1,5 benzodiazepine derivatives | |
IE37288B1 (en) | Pharmaceutical compositions for use in the treatment of certain respiratory diseases or conditions in prematurely born children | |
KR0150182B1 (ko) | 소염제로서의 7-치환 아미노-8-치환 카르보닐-메틸 아미노-1-옥사스피로(4,5)데칸 |
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 |