BR0011125A - Polimorfos de citrato de (2-benzidril-1-azabiciclo[2.2.2]oct-3-il)-(5-iso-propil-2-m etoxibenzil)-amina cristalino como antagonistas de receptor nk-1 - Google Patents
Polimorfos de citrato de (2-benzidril-1-azabiciclo[2.2.2]oct-3-il)-(5-iso-propil-2-m etoxibenzil)-amina cristalino como antagonistas de receptor nk-1Info
- Publication number
- BR0011125A BR0011125A BR0011125-2A BR0011125A BR0011125A BR 0011125 A BR0011125 A BR 0011125A BR 0011125 A BR0011125 A BR 0011125A BR 0011125 A BR0011125 A BR 0011125A
- Authority
- BR
- Brazil
- Prior art keywords
- benzhydryl
- oct
- polymorphs
- methoxybenzyl
- iso
- Prior art date
Links
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 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
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 title 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 title 1
- -1 oct-3-yl Chemical group 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- YASYEJJMZJALEJ-UHFFFAOYSA-N Citric acid monohydrate Chemical compound O.OC(=O)CC(O)(C(O)=O)CC(O)=O YASYEJJMZJALEJ-UHFFFAOYSA-N 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 239000002775 capsule Substances 0.000 abstract 1
- 238000002512 chemotherapy Methods 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 238000001990 intravenous administration Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000004682 monohydrates Chemical class 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
Patente de Invenção: "POLIMORFOS DE CITRATO DE (2-BENZIDRIL-1-AZABICICLO[2.2.2]OCT-3-IL)-(5-ISO-PROPIL-2-M ETOXIBENZIL)-AMINA CRISTALINO COMO ANTAGONISTAS DE RECEPTOR NK-1". Duas formas crístalinas polimórficas do mono-hidrato do citrato de (2-benzidril-1-azo-biciclo[2.2.2]oct-3-il)-(5-isopropil-2-metoxibenzil)-a mina (os mono-hidratos) são a Forma A e Forma B. A composição farmacêutica contendo pelo menos um destes polimorfos tem estabilidade vantajosa para formulação para tratar emesis aguda em pacientes recebendo quimioterapia. A administração desta composição farmacêutica é convencionalmente oral, por meio de, preferencialmente, comprimido ou cápsula, e intravenosa. Um método para fazer as Formas A e B é também revelado.
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 (1)
| Publication Number | Publication Date |
|---|---|
| BR0011125A true BR0011125A (pt) | 2002-02-19 |
Family
ID=22475353
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0011125-2A BR0011125A (pt) | 1999-06-01 | 2000-05-17 | Polimorfos de citrato de (2-benzidril-1-azabiciclo[2.2.2]oct-3-il)-(5-iso-propil-2-m etoxibenzil)-amina cristalino como antagonistas de receptor nk-1 |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US6387925B1 (pt) |
| EP (1) | EP1181289A1 (pt) |
| JP (1) | JP2003501353A (pt) |
| KR (1) | KR20020005055A (pt) |
| CN (1) | CN1353712A (pt) |
| AP (1) | AP2001002350A0 (pt) |
| AR (1) | AR029753A1 (pt) |
| AU (1) | AU767331B2 (pt) |
| BG (1) | BG106139A (pt) |
| BR (1) | BR0011125A (pt) |
| CA (1) | CA2372236A1 (pt) |
| CO (1) | CO5170468A1 (pt) |
| CR (1) | CR6513A (pt) |
| CZ (1) | CZ20014270A3 (pt) |
| DZ (1) | DZ3051A1 (pt) |
| EA (1) | EA004206B1 (pt) |
| EE (1) | EE200100655A (pt) |
| GT (1) | GT200000086A (pt) |
| HK (1) | HK1046407A1 (pt) |
| HN (1) | HN2000000076A (pt) |
| HR (1) | HRP20010884A2 (pt) |
| HU (1) | HUP0201798A3 (pt) |
| IL (1) | IL145952A0 (pt) |
| IS (1) | IS6129A (pt) |
| MX (1) | MXPA01012328A (pt) |
| NO (1) | NO20015845L (pt) |
| NZ (1) | NZ514762A (pt) |
| OA (1) | OA11955A (pt) |
| PA (1) | PA8496001A1 (pt) |
| PE (1) | PE20010155A1 (pt) |
| PL (1) | PL352715A1 (pt) |
| SK (1) | SK17342001A3 (pt) |
| SV (1) | SV2002000092A (pt) |
| TN (1) | TNSN00119A1 (pt) |
| TR (1) | TR200103472T2 (pt) |
| UY (1) | UY26177A1 (pt) |
| WO (1) | WO2000073303A1 (pt) |
| ZA (1) | ZA200109839B (pt) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004031191A1 (en) * | 2002-10-04 | 2004-04-15 | Merck Sharp & Dohme Limited | Azabicyclic spiroether derivatives as receptor antagonists |
| EP1726583A3 (en) * | 2003-06-18 | 2007-05-09 | Teva Pharmaceutical Industries Ltd | Fluvastatin sodium crystal form LXXIX, processes for preparing it, compositions containing it and methods of using it. |
| 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 |
| KR100214905B1 (ko) * | 1991-05-31 | 1999-08-02 | 디. 제이. 우드, 스피겔 알렌 제이 | 퀴누클리딘 유도체 |
| 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 |
| 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 IL IL14595200A patent/IL145952A0/xx unknown
- 2000-05-17 OA OA1200100317A patent/OA11955A/en unknown
- 2000-05-17 CZ CZ20014270A patent/CZ20014270A3/cs unknown
- 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 EE EEP200100655A patent/EE200100655A/xx unknown
- 2000-05-17 PL PL00352715A patent/PL352715A1/xx not_active Application Discontinuation
- 2000-05-17 NZ NZ514762A patent/NZ514762A/xx unknown
- 2000-05-17 AP APAP/P/2001/002350A patent/AP2001002350A0/en unknown
- 2000-05-17 MX MXPA01012328A patent/MXPA01012328A/es not_active Application Discontinuation
- 2000-05-17 KR KR1020017015324A patent/KR20020005055A/ko not_active Application Discontinuation
- 2000-05-17 WO PCT/IB2000/000663 patent/WO2000073303A1/en not_active Application Discontinuation
- 2000-05-17 TR TR2001/03472T patent/TR200103472T2/xx unknown
- 2000-05-17 BR BR0011125-2A patent/BR0011125A/pt not_active IP Right Cessation
- 2000-05-17 CN CN00808340A patent/CN1353712A/zh active Pending
- 2000-05-17 AU AU44246/00A patent/AU767331B2/en not_active Ceased
- 2000-05-17 CA CA002372236A patent/CA2372236A1/en not_active Abandoned
- 2000-05-17 EP EP00925526A patent/EP1181289A1/en not_active Withdrawn
- 2000-05-17 HN HN2000000076A patent/HN2000000076A/es unknown
- 2000-05-17 SK SK1734-2001A patent/SK17342001A3/sk unknown
- 2000-05-17 JP JP2001500628A patent/JP2003501353A/ja active Pending
- 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 TN TNTNSN00119A patent/TNSN00119A1/fr unknown
- 2000-05-31 SV SV2000000092A patent/SV2002000092A/es 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
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 6A, 7A E 8A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO PUBLICADO NA RPI 1962 DE 12/08/2008. |