Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
  • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
  • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• • 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
  • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• • 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
  • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P25/16—Anti-Parkinson drugs
• • 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
  • A61P25/22—Anxiolytics
• • 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
  • A61P25/24—Antidepressants
• • 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

Definitions

• the present invention relates to a novel compound, to processes for preparing it and to its use in treating medical disorders.
• paroxetine ascorbate According to the present invention there is provided paroxetine ascorbate.
• novel salt of this invention is provided in non-crystalline form, which may a solid or an oil.
• the oil is preferably absorbed on a solid carrier, especially a carrier that is usable as a component of a pharmaceutical composition
• novel salt of this invention is provided in crystalline form.
• each polymorph forms another aspect of this invention.
• Paroxetine ascorbate may be prepared by contacting stoichiometric amounts of ascorbic acid and paroxetine free base.
• the acid or base is in solution, more preferably both are in solution. Elevated temperature may be used to bring the acid into solution, but good yields of the salt are obtained by evaporation of some or all of the solvent or by controlled cooling, preferably in stages.
• Most commonly used solvents are suitable for mobilizing paroxetine free base, for example toluene, alcohols such as
• Suitable solvents for ascorbic acid include water and lower alcohols.
• the salt may be isolated in solid form by conventional means from a solution thereof obtained as above.
• the non-crystalline salt may be prepared by precipitation, spray drying, and freeze drying of solutions, or vacuum drying of oils, or solidification of melts obtained from reaction of the free base and the acid.
• the crystalline salt may be prepared by crystallization or recrystallization from appropriate solvents.
• Solvates may be returned to the unsolvated salt by heating, for example by oven-drying, or by treatment with a displacement solvent which does not form a solvate.
• water Prior to the isolation of the paroxetine salt, water may be removed by azeotropic distillation to avoid the formation of hydrates or to obtain the product in anhydrous form.
• suitable solvents for the solution of the salt are those which form an azeotrope with water such as toluene and propan-2-ol. It should also be appreciated that mixtures of solvents can also be used to aid the azeotropic removal of water.
• crystallization may be carried out from any solvent which allows formation of the desired crystal structure, using seeds of the desired structure where necessary or desirable.
• individual polymo ⁇ hs are preferably crystallized directly from a solution of the salt, although recrystallizing a solution of one polymo ⁇ h using seeds of another polymo ⁇ h may also be carried out.
• Paroxetine free base may be prepared according to the procedures generally outlined in US Patent No 4,007,196 and EP-B-0 223403. Ascorbic acid is commercially available.
• the compounds of this invention may be used to treat and prevent the following disorders:
• the Disorders are herein after referred to as "the Disorders”.
• the present invention further provides a method for treating and/or preventing any one or more of the Disorders by administering an effective and/or prophylactic amount of a salt of the invention to a sufferer in need thereof.
• the present invention further provides a pharmaceutical composition for use in the treatment and/or prevention of the Disorders which comprises an admixture of a salt of the invention with a pharmaceutically acceptable carrier.
• the present invention also provides the use of a salt of the invention for treating and/or preventing the Disorders.
• the present invention also provides the use of a salt of the invention in the manufacture of a medicament for treating and/or preventing the Disorders.
• the present invention is applied to the treatment of depression, OCD and panic.
• compositions of this invention are usually adapted for oral administration, but formulations for dissolution for parental administration are also within the scope of this invention.
• the composition is usually presented as a unit dose composition containing from 1 to 200mg of active ingredient calculated on a free base basis, more usually from 5 to lOOmg, for example 10 to 50mg such as 10, 12.5, 15, 20, 25, 30 or 40mg by a human patient. Most preferably unit doses contain 20mg of active ingredient calculated on a free base basis. Such a composition is normally taken from 1 to 6 times daily, for example 2, 3 or 4 times daily so that the total amount of active agent administered is within the range 5 to 400mg of active ingredient calculated on a free base basis. Most preferably the unit dose is taken once a day.
• Preferred unit dosage forms include tablets or capsules.
• compositions of this invention may be formulated by conventional methods of admixture such as blending, filling and compressing.
• Suitable carriers for use in this invention include a diluent, a binder, a disintegrant, a colouring agent, a flavouring agent and/or preservative. These agents may be utilized in conventional manner, for example in a manner similar to that already used for marketed anti-depressant agents.
• compositions include those described EP-B-0- 223403, and US 4,007,196 in which the products of the present invention may be used as the active ingredients.
• Example 1 Preparation of paroxetine ascorbate
• the tablets are made satisfactorily on a single punch or a Rotary press.
• Dihydrate are screened and mixed together in a suitable mixer.

Applications Claiming Priority (3)

Publications (1)

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Family Applications (1)

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• 1998
  • 1998-04-25 GB GBGB9808896.6A patent/GB9808896D0/en not_active Ceased
• 1999
  • 1999-04-23 SK SK1591-2000A patent/SK15912000A3/sk unknown
  • 1999-04-23 AU AU36184/99A patent/AU3618499A/en not_active Abandoned
  • 1999-04-23 KR KR1020007011809A patent/KR20010042977A/ko not_active Application Discontinuation
  • 1999-04-23 WO PCT/GB1999/001244 patent/WO1999055698A1/en not_active Application Discontinuation
  • 1999-04-23 ID IDW20002168A patent/ID26083A/id unknown
  • 1999-04-23 BR BR9909868-7A patent/BR9909868A/pt not_active Application Discontinuation
  • 1999-04-23 EA EA200001104A patent/EA200001104A1/ru unknown
  • 1999-04-23 TR TR2000/03084T patent/TR200003084T2/tr unknown
  • 1999-04-23 CN CN99805160A patent/CN1297448A/zh active Pending
  • 1999-04-23 PL PL99343677A patent/PL343677A1/xx not_active Application Discontinuation
  • 1999-04-23 IL IL13908199A patent/IL139081A0/xx unknown
  • 1999-04-23 CA CA002330055A patent/CA2330055A1/en not_active Abandoned
  • 1999-04-23 AP APAP/P/2000/001963A patent/AP2000001963A0/en unknown
  • 1999-04-23 JP JP2000545858A patent/JP2002513019A/ja active Pending
  • 1999-04-23 ID IDW20002169A patent/ID26654A/id unknown
  • 1999-04-23 EP EP99918151A patent/EP1089995A1/en not_active Withdrawn
  • 1999-04-23 HU HU0102116A patent/HUP0102116A3/hu unknown
• 2000
  • 2000-10-23 ZA ZA200005912A patent/ZA200005912B/en unknown
  • 2000-10-24 NO NO20005352A patent/NO20005352D0/no not_active Application Discontinuation
  • 2000-11-13 BG BG104940A patent/BG104940A/bg unknown

Non-Patent Citations (1)

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