PE12598A1 - ZWITTERIONIC FORMS OF TROVAFLOXACIN - Google Patents
ZWITTERIONIC FORMS OF TROVAFLOXACINInfo
- Publication number
- PE12598A1 PE12598A1 PE1996000633A PE00063396A PE12598A1 PE 12598 A1 PE12598 A1 PE 12598A1 PE 1996000633 A PE1996000633 A PE 1996000633A PE 00063396 A PE00063396 A PE 00063396A PE 12598 A1 PE12598 A1 PE 12598A1
- Authority
- PE
- Peru
- Prior art keywords
- trovafloxacin
- obtaining
- pentahydrate
- dry
- main peaks
- Prior art date
Links
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Physical Water Treatments (AREA)
- Processing Of Solid Wastes (AREA)
Abstract
CARACTERIZADAS PORQUE COMPRENDEN: 1) POLIMORFO P(I), NO HIGROSCOPICO; 2) POLIMORFO P(II), HIGROSCOPICO; 3) PENTAHIDRATO; CUYOS PATRONES DE DIFRACCION DE RAYOS X DE POLVO, COMPRENDEN PARA: 1) P(I), 15 PICOS PRINCIPALES, DE 6,9� 2U(Cu) A 26,3� 2U(Cu); 2) P(II), 8 PICOS PRINCIPALES, DE 8,4� 2U(Cu) A 26,1� 2U(Cu); 3) PENTAHIDRATO, 17 PICOS PRINCIPALES DE 6,6� 2U(Cu) A 29,5� 2U(Cu). TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LA FORMA METAESTABLE DEL ZWITTERION DE TROVAFLOXACINA, DE FORMULA (I), QUE COMPRENDE: A) TRATAR LA SAL ACIDA DE TROVAFLOXACINA CON UNA BASE HASTA UN pH DE 7,5 A 8,5 Y A UNA TEMPERATURA ELEVADA; O B) RETIRAR LOS GRUPO PROTECTOR AMINO Y/O CARBOXILO, OPCIONALMENTE PRESENTES EN LA TROVAFLOXACINA. ADEMAS SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LAS FORMAS ZWITTERIONICAS DE TROVAFLOXACINA, QUE COMPRENDEN: 1) TRATAR LA SOLUCION ACUOSA DE LA FORMA METAESTABLE CON: a) UN DISOLVENTE POLAR, LUEGO (d), OBTENIENDO P(I); b) UN DISOLVENTE APOLAR, LUEGO (d), OBTENIENDO P(II); c) AGUA, LUEGO (e), OBTENIENDO EL PENTAHIDRATO; d) ELIMINAR AZEOTROPICAMENTE EL AGUA RESIDUAL Y SECAR AL VACIO; e) SECAR CON AIRE CALIENTE, ELIMINAR LAS AGUAS MADRES Y SECAR A TEMPERATURA AMBIENTE; 2) TRATAR P(II) CON UN DISOLVENTE POLAR A REFLUJO, OBTENIENDO P(I). SON ANTIBIOTICOS PARA BACTERIAS GRAM POSITIVASCHARACTERIZED BECAUSE THEY INCLUDE: 1) POLYMORPH P (I), NON-HYGROSCOPIC; 2) POLYMORPH P (II), HYGROSCOPIC; 3) PENTAHYDRATE; WHOSE X-RAY DUST DRAWING PATTERNS, INCLUDE: 1) P (I), 15 MAIN PEAKS, FROM 6.9� 2U (Cu) TO 26.3� 2U (Cu); 2) P (II), 8 MAIN PEAKS, FROM 8.4� 2U (Cu) TO 26.1� 2U (Cu); 3) PENTAHYDRATE, 17 MAIN PEAKS FROM 6.6� 2U (Cu) TO 29.5� 2U (Cu). IT ALSO REFERS TO THE PROCEDURE FOR THE PREPARATION OF THE METASTABLE FORM OF ZWITTERION OF TROVAFLOXACIN, OF FORMULA (I), WHICH INCLUDES: A) TREATING THE ACIDED SALT OF TROVAFLOXACIN WITH A BASE UP TO A pH OF 7.5 TO 8.5 AND AT A TEMPERATURE HIGH; OR B) REMOVE THE AMINO AND / OR CARBOXYL PROTECTIVE GROUP, OPTIONALLY PRESENT IN TROVAFLOXACIN. IT FURTHER REFERS TO THE PROCEDURE FOR THE PREPARATION OF THE ZWITTERIONIC FORMS OF TROVAFLOXACIN, WHICH INCLUDE: 1) TREAT THE AQUEOUS SOLUTION OF THE META-STABLE FORM WITH: a) A POLAR SOLVENT, THEN (d), OBTAINING P (I); b) AN APOLAR SOLVENT, THEN (d), OBTAINING P (II); c) WATER, THEN (e), OBTAINING THE PENTAHYDRATE; d) ELIMINATE AZEOTROPICALLY THE RESIDUAL WATER AND DRY IN A VACUUM; e) DRY WITH HOT AIR, ELIMINATE THE MOTHER WATERS AND DRY AT ROOM TEMPERATURE; 2) TREAT P (II) WITH A POLAR SOLVENT AT REFLUX, OBTAINING P (I). THEY ARE ANTIBIOTICS FOR GRAM POSITIVE BACTERIA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US297595P | 1995-08-29 | 1995-08-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE12598A1 true PE12598A1 (en) | 1998-03-20 |
Family
ID=21703460
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1996000633A PE12598A1 (en) | 1995-08-29 | 1996-08-26 | ZWITTERIONIC FORMS OF TROVAFLOXACIN |
Country Status (30)
| Country | Link |
|---|---|
| EP (1) | EP0850060A1 (en) |
| JP (1) | JP3188476B2 (en) |
| KR (1) | KR100343909B1 (en) |
| CN (1) | CN1190889A (en) |
| AP (1) | AP636A (en) |
| AR (1) | AR003985A1 (en) |
| AU (1) | AU704115B2 (en) |
| BR (1) | BR9609998A (en) |
| CA (1) | CA2229786C (en) |
| CO (1) | CO4480739A1 (en) |
| CZ (1) | CZ56698A3 (en) |
| DZ (1) | DZ2087A1 (en) |
| GT (1) | GT199600072A (en) |
| HR (1) | HRP960395B1 (en) |
| HU (1) | HUP9900170A3 (en) |
| IL (1) | IL122651A (en) |
| MA (1) | MA23966A1 (en) |
| MY (1) | MY113874A (en) |
| NO (1) | NO309814B1 (en) |
| NZ (1) | NZ312199A (en) |
| OA (1) | OA10669A (en) |
| PE (1) | PE12598A1 (en) |
| PL (1) | PL325170A1 (en) |
| RU (1) | RU2144921C1 (en) |
| SK (1) | SK23898A3 (en) |
| TN (1) | TNSN96109A1 (en) |
| TR (1) | TR199800339T1 (en) |
| WO (1) | WO1997007800A1 (en) |
| YU (1) | YU48396A (en) |
| ZA (1) | ZA967282B (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HN1998000106A (en) | 1997-08-01 | 1999-01-08 | Pfizer Prod Inc | PARENTERAL COMPOSITIONS OF ALATROFLAXACINO |
| US7019142B2 (en) | 1998-01-16 | 2006-03-28 | Pfizer Inc. | Process for preparing naphthyridones and intermediates |
| PA8466701A1 (en) * | 1998-01-21 | 2000-09-29 | Pfizer Prod Inc | TROVAFLOXACINO MESYLATE TABLET |
| US6114531A (en) * | 1998-07-28 | 2000-09-05 | Pfizer Inc. | Process for preparing quinolone and naphthyridone carboxylic acids |
| HN1999000141A (en) * | 1998-09-03 | 2000-06-19 | Pfizer Prod Inc | PROCEDURE FOR PREPARING SALTS OF TROVAFLOXACIN FOR ADDITION OF ACIDS. |
| US6239141B1 (en) * | 1999-06-04 | 2001-05-29 | Pfizer Inc. | Trovafloxacin oral suspensions |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5164402A (en) * | 1989-08-16 | 1992-11-17 | Pfizer Inc | Azabicyclo quinolone and naphthyridinone carboxylic acids |
-
1996
- 1996-07-29 KR KR10-1998-0701468A patent/KR100343909B1/en not_active IP Right Cessation
- 1996-07-29 BR BR9609998A patent/BR9609998A/en unknown
- 1996-07-29 TR TR1998/00339T patent/TR199800339T1/en unknown
- 1996-07-29 RU RU98103873/04A patent/RU2144921C1/en not_active IP Right Cessation
- 1996-07-29 AU AU63676/96A patent/AU704115B2/en not_active Ceased
- 1996-07-29 CA CA002229786A patent/CA2229786C/en not_active Expired - Fee Related
- 1996-07-29 EP EP96923020A patent/EP0850060A1/en not_active Withdrawn
- 1996-07-29 HU HU9900170A patent/HUP9900170A3/en unknown
- 1996-07-29 NZ NZ312199A patent/NZ312199A/en unknown
- 1996-07-29 JP JP50343697A patent/JP3188476B2/en not_active Expired - Fee Related
- 1996-07-29 CZ CZ98566A patent/CZ56698A3/en unknown
- 1996-07-29 SK SK238-98A patent/SK23898A3/en unknown
- 1996-07-29 IL IL12265196A patent/IL122651A/en not_active IP Right Cessation
- 1996-07-29 WO PCT/IB1996/000756 patent/WO1997007800A1/en not_active Application Discontinuation
- 1996-07-29 CN CN96195624A patent/CN1190889A/en active Pending
- 1996-07-29 PL PL96325170A patent/PL325170A1/en unknown
- 1996-08-23 GT GT199600072A patent/GT199600072A/en unknown
- 1996-08-26 PE PE1996000633A patent/PE12598A1/en not_active Application Discontinuation
- 1996-08-26 AR ARP960104121A patent/AR003985A1/en unknown
- 1996-08-28 MY MYPI96003579A patent/MY113874A/en unknown
- 1996-08-28 MA MA24344A patent/MA23966A1/en unknown
- 1996-08-28 TN TNTNSN96109A patent/TNSN96109A1/en unknown
- 1996-08-28 ZA ZA9607282A patent/ZA967282B/en unknown
- 1996-08-28 DZ DZ960131A patent/DZ2087A1/en active
- 1996-08-28 YU YU48396A patent/YU48396A/en unknown
- 1996-08-29 AP APAP/P/1996/000853A patent/AP636A/en active
- 1996-08-29 CO CO96046149A patent/CO4480739A1/en unknown
- 1996-08-29 HR HR960395A patent/HRP960395B1/en not_active IP Right Cessation
-
1998
- 1998-02-27 NO NO980862A patent/NO309814B1/en not_active Application Discontinuation
- 1998-02-27 OA OA9800026A patent/OA10669A/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |