BR0313231A - sal e polimorfos de hemifumarato de desloratadina - Google Patents
sal e polimorfos de hemifumarato de desloratadinaInfo
- Publication number
- BR0313231A BR0313231A BRPI0313231-5A BR0313231A BR0313231A BR 0313231 A BR0313231 A BR 0313231A BR 0313231 A BR0313231 A BR 0313231A BR 0313231 A BR0313231 A BR 0313231A
- Authority
- BR
- Brazil
- Prior art keywords
- desloratadine
- polymorphic
- temperature
- mixing
- polymorphs
- Prior art date
Links
- JAUOIFJMECXRGI-UHFFFAOYSA-N Neoclaritin Chemical compound C=1C(Cl)=CC=C2C=1CCC1=CC=CN=C1C2=C1CCNCC1 JAUOIFJMECXRGI-UHFFFAOYSA-N 0.000 title abstract 5
- 229960001271 desloratadine Drugs 0.000 title abstract 5
- 150000003839 salts Chemical class 0.000 title abstract 4
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 238000001914 filtration Methods 0.000 abstract 2
- 239000001530 fumaric acid Substances 0.000 abstract 2
- 238000003756 stirring Methods 0.000 abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 2
- -1 4-piperidylidene Chemical group 0.000 abstract 1
- 208000006278 hypochromic anemia Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
"SAL E POLIMORFOS DE HEMIFUMARATO DE DESLORATAINA". A presente invenção refere-se a um processo de preparação de novos sais de hemifumarato polimórficos de 8-cloros-6,11-diidro-11(4-piperidilideno)-5h-benzo¢5,6!-cicloepta¢1,2- b!piridina, em seguida chamada "desloratadina". Estas formas polimórficas de sal apresentam solubilidade muito mais elevada em água e também em solventes orgânicos se comparam à desloratadina de origem. O processo de preparação das formas polimórficas compreendendo:a) misturar a solução etanólica de desloratadina e ácido fumárico em um temperatura de cerca de 55°C a 70°C, e agitar por 30 a 45 minutos após a mistura, e depois disso filtrar o sólido assim preparado na condição quente; para produzir a forma polimórfica 2 tendo uma DSC de 232°C + 2°; ou b) misturar a solução etanólica de desloratadina e ácido fumárico em uma temperatura de cerca de 15°C à temperatura ambiente (25°C) e agitar nesta temperatura por 30 a 45 minutos, depois filtrar em temperatura ambiente; para produzir a forma polimórfica 1 dendo uma DSC de 224°C + 2° C.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40115302P | 2002-08-05 | 2002-08-05 | |
| PCT/US2003/022312 WO2004012738A1 (en) | 2002-08-05 | 2003-07-17 | Novel salt and polymorphs of desloratadine hemifumarate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0313231A true BR0313231A (pt) | 2007-07-24 |
Family
ID=31495932
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0313231-5A BR0313231A (pt) | 2002-08-05 | 2003-07-17 | sal e polimorfos de hemifumarato de desloratadina |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US6962924B2 (pt) |
| EP (1) | EP1539161A1 (pt) |
| JP (1) | JP2005539010A (pt) |
| KR (1) | KR20050069976A (pt) |
| CN (1) | CN1674901A (pt) |
| AU (1) | AU2003251974C1 (pt) |
| BR (1) | BR0313231A (pt) |
| CA (1) | CA2494288A1 (pt) |
| EC (1) | ECSP055580A (pt) |
| HR (1) | HRP20050110A2 (pt) |
| IL (1) | IL166289A0 (pt) |
| MX (1) | MXPA05001470A (pt) |
| NO (1) | NO20051166L (pt) |
| PL (1) | PL374799A1 (pt) |
| RU (1) | RU2005106205A (pt) |
| WO (1) | WO2004012738A1 (pt) |
| ZA (1) | ZA200500372B (pt) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040242619A1 (en) * | 2003-03-12 | 2004-12-02 | Toth Zoltan G. | Processes for preparation of polymorphic forms of desloratadine |
| CZ200798A3 (cs) * | 2004-07-07 | 2007-06-20 | Egis Gyogyszergyár Nyrt. | Nový pseudopolymorf desloratadinu vytvorený s oxidem uhlicitým |
| CA2541045A1 (en) * | 2006-03-24 | 2007-09-24 | Pharmascience Inc. | A descarbonylethoxyloratadine containing pharmaceutical composition |
| US20090082385A1 (en) * | 2007-09-26 | 2009-03-26 | Protia, Llc | Deuterium-enriched desloratidine |
| CN110638750B (zh) * | 2019-10-28 | 2021-08-27 | 深圳市贝美药业有限公司 | 一种地氯雷他定药物的制备方法及其制剂 |
| CN113081958B (zh) * | 2021-05-01 | 2022-05-03 | 安徽新世纪药业有限公司 | 一种地氯雷他定口服溶液及其制备方法 |
| CN115785065A (zh) * | 2022-12-02 | 2023-03-14 | 山东达因海洋生物制药股份有限公司 | 一种地氯雷他定共晶及其制备方法与应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61501205A (ja) | 1984-02-15 | 1986-06-19 | シェリング・コ−ポレ−ション | ８↓−クロル↓−６，１１↓−ジヒドロ↓−１１↓−（４↓−ピペリジリデン）↓−５Ｈ↓−ベンゾ〔５，６〕シクロヘプタ〔１，２−ｂ〕ピリジンおよびその塩、これらの化合物の製造方法、ならびにこれらの化合物を含有する医薬組成物 |
| FR2639942B1 (fr) * | 1988-12-02 | 1991-03-29 | Sanofi Sa | Ethers oximes de propenone, procede pour leur preparation et compositions pharmaceutiques les contenant |
| US4954503A (en) * | 1989-09-11 | 1990-09-04 | Hoechst-Roussel Pharmaceuticals, Inc. | 3-(1-substituted-4-piperazinyl)-1H-indazoles |
| DK0750616T3 (da) * | 1994-03-16 | 2001-07-23 | Cenes Ltd | Syreadditionssalte af 2,3,4,5-tetrahydro-1H-3-benzazapinforbindelser |
| US5595997A (en) | 1994-12-30 | 1997-01-21 | Sepracor Inc. | Methods and compositions for treating allergic rhinitis and other disorders using descarboethoxyloratadine |
| US6506767B1 (en) * | 1997-07-02 | 2003-01-14 | Schering Corporation | 8-chloro-6,11-dihydro-11-(4-piperidylidine)-5H-benzo[5,6]cyclohepta[1-2-b] pyridine |
| UA62976C2 (en) | 1997-07-02 | 2004-01-15 | Schering Corp | Polymorphs of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5h-benzo[5,6]cyclohepta[1,2-b]pyridine |
| US6335347B1 (en) | 1997-10-10 | 2002-01-01 | Schering Corporation | Ethyl 4-(8-chloro-5,6-dihydro-11 H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidene carboxylate polymorph |
| JP2001519428A (ja) * | 1997-10-10 | 2001-10-23 | シェーリング コーポレイション | エチル４−（８−クロロ−５，６−ジヒドロ−１１Ｈ−ベンゾ［５，６］シクロヘプタ［１，２−ｂ］ピリジン−１１−イリデン）−１−ピペリデンカルボキシレート多形物 |
| US6100274A (en) | 1999-07-07 | 2000-08-08 | Schering Corporation | 8-chloro-6,11-dihydro-11- ](4-piperidylidine)-5H-benzo[5,6]cyclohepta[1,2-bpyridine oral compositions |
| HU226998B1 (en) * | 2000-11-23 | 2010-04-28 | Richter Gedeon Nyrt | Desloratadine hemisulphate, process for the preparation thereof and pharmaceutical compositions containing the same |
-
2003
- 2003-07-17 BR BRPI0313231-5A patent/BR0313231A/pt not_active IP Right Cessation
- 2003-07-17 AU AU2003251974A patent/AU2003251974C1/en not_active Ceased
- 2003-07-17 PL PL03374799A patent/PL374799A1/xx not_active Application Discontinuation
- 2003-07-17 CN CNA038188368A patent/CN1674901A/zh active Pending
- 2003-07-17 WO PCT/US2003/022312 patent/WO2004012738A1/en not_active Ceased
- 2003-07-17 US US10/621,670 patent/US6962924B2/en not_active Expired - Fee Related
- 2003-07-17 KR KR1020057002075A patent/KR20050069976A/ko not_active Withdrawn
- 2003-07-17 CA CA002494288A patent/CA2494288A1/en not_active Abandoned
- 2003-07-17 JP JP2004526119A patent/JP2005539010A/ja active Pending
- 2003-07-17 MX MXPA05001470A patent/MXPA05001470A/es unknown
- 2003-07-17 RU RU2005106205/04A patent/RU2005106205A/ru not_active Application Discontinuation
- 2003-07-17 HR HR20050110A patent/HRP20050110A2/xx not_active Application Discontinuation
- 2003-07-17 EP EP03766873A patent/EP1539161A1/en not_active Withdrawn
-
2005
- 2005-01-13 IL IL16628905A patent/IL166289A0/xx unknown
- 2005-01-14 ZA ZA200500372A patent/ZA200500372B/en unknown
- 2005-01-26 EC EC2005005580A patent/ECSP055580A/es unknown
- 2005-03-04 NO NO20051166A patent/NO20051166L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20050069976A (ko) | 2005-07-05 |
| US20040058949A1 (en) | 2004-03-25 |
| NO20051166L (no) | 2005-03-04 |
| MXPA05001470A (es) | 2005-09-30 |
| JP2005539010A (ja) | 2005-12-22 |
| PL374799A1 (en) | 2005-10-31 |
| AU2003251974B2 (en) | 2006-04-27 |
| AU2003251974A1 (en) | 2004-02-23 |
| US6962924B2 (en) | 2005-11-08 |
| WO2004012738A1 (en) | 2004-02-12 |
| RU2005106205A (ru) | 2005-12-10 |
| AU2003251974C1 (en) | 2006-09-14 |
| CN1674901A (zh) | 2005-09-28 |
| CA2494288A1 (en) | 2004-02-12 |
| EP1539161A1 (en) | 2005-06-15 |
| HRP20050110A2 (en) | 2006-02-28 |
| IL166289A0 (en) | 2006-01-15 |
| ECSP055580A (es) | 2005-04-18 |
| ZA200500372B (en) | 2006-07-26 |
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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 5A, 6A E 7A ANUIDADE(S). |
|
| 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 8.6 PUBLICADO NA RPI 2064 DE 27/07/2010. |