U.S. patents available from 1976 to present.
U.S. patent applications available from 2005 to present.

Dispersible compositions containing L-DOPA ethyl ester

Patent 6376545 Issued on April 23, 2002. Estimated Expiration Date: Icon_subject November 10, 2019. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

3803120

3885026

Novel, transient pro-drug forms of l-dopa useful in the treatment of parkinson's disease
Patent #: 3939253
Issued on: 02/17/1976
Inventor: Bodor ,   et al.

Effervescent enteric coated L-dopa formulation and method of using the same
Patent #: 3961041
Issued on: 06/01/1976
Inventor: Nishimura ,   et al.

Novel, transient pro-drug forms of L-DOPA to treat Parkinson's disease
Patent #: 4035507
Issued on: 07/12/1977
Inventor: Bodor ,   et al.

Rectally absorbable form of L-dopa
Patent #: 4663349
Issued on: 05/05/1987
Inventor: Repta

Rectally absorbable form of L-dopa
Patent #: 4771073
Issued on: 09/13/1988
Inventor: Repta

Pharmaceutical compositions containing levodopa methyl ester, preparation and therapeutic applications thereof
Patent #: 4826875
Issued on: 05/02/1989
Inventor: Chiesi

Method of treating parkinson's syndrome
Patent #: 4916151
Issued on: 04/10/1990
Inventor: Bey, et al.

Process for preparing ethyl ester of L-DOPA
Patent #: 5354885
Issued on: 10/11/1994
Inventor: Milman, et al.

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Inventor

Assignee

Application

No. 437699 filed on 11/10/1999

US Classes:

514/567, Benzene ring nonionically bonded514/538, Nitrogen bonded to carbon in Z moiety514/614, N-N containing (e.g., aminimine, hydrazine, etc.)514/654, The chain consists of two or more carbons which are unsubtituted or have acyclic hydrocarbyl substituents only514/657, Bicyclo ring system514/960SIGNIFICANT, TABLET FORMULATION (E.G., DESIGNATED EXCIPIENT, DISINTEGRANT, GLYDENT OR LUBRICANT, ETC.)

Examiners

Primary: Krass, Frederick
Assistant: Jagoe, Donna

Attorney, Agent or Firm

Foreign Patent References

  • 522128 EP. 01/12/1992
  • 1364505 GB. 08/12/1974

International Classes

A61K 031/195
A61K 031/24
A61K 031/16
A61K 031/135

Abstract

The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase inhibitor, a filler, a disintegrant, and a lubricant. The present invention also provides a method of preparing the pharmaceutical composition described herein.

Other References

  • Remington's Pharmaceutical Sciences, 1975, Mac Publishing Co. 15th ediction, chapter 89, pp. 1576 to 1607.
  • Banerjee et al., "Derivatives of 3,4-Dihydroxyphenylalanine for Peptide Synthesis" J. Org. Chem. (1976) 41(18):3056-3058 (Exhibit 14)
  • Bodor et al., "Improved Delivery Through Biological Membranes. 4. Prodrugs of L-DOPA" Journal of Medicinal Chemistry (1977) 20(11): 1435-1445 (Exhibit 15)
  • Cooper et al., "L-DOPA Methyl Ester--A Candidate for Chronic Systemic Delivery of L-DOPA in Parkinson's Disease" Clin. Neuropharmacol. (1984) 7:(1) 89-98 (Exhibit 16)
  • Cooper et al., "L-DOPA Esters as Potential Prodrugs: Behavioural Acitivity in Experimentation Models of Parkinson's Disease" J. Pharm Pharmacol (Aug. 1987) 39(8): 627-635 (Exhibit 17)
  • El-Naggar et al., "Synthesis of Some Dipeptides Containing 2-Aminobutyric Acid, 3,4-Dihydroxyphenylalanine, Urea and Thiourea Derivatives" Polish Journal of Chemistry (1978) 52:1809-1814 (Exhibit 18)
  • Fix et al., "Short-Chain Alkyl Esters of L-DOPA as Prodrugs for Rectal Absorption" Pharm. Res. (1989) 6(6): 501-505 (Exhibit 19)
  • Juncos et al., "Levodopa Methyl Ester Treatment of Parkinson's Disease" Neurology (1987) 37: 1242-1245 (Exhibit 20)
  • Lai et al., New Compounds: Synthesis of Alkyl Esters of D,L-DOPA, J. Phar. Sci. (1973) 62: 510-511 (Exhibit 21)
  • Lou et al., "Direct Enantiomer Separation of Phenylalanine, DOPA and Their Intermediates by Supercritical Fluid Chromatography" Journal of Chromatography (1992) 605: 103-107 (Exhibit 22)
  • Marrel et al., "L-DOPA Esters as Potential Prodrugs" Eur. J. Med. Chem. (1985) 20(5): 459-465 (Exhibit 23)
  • Tomiuchi et al., "Enzymatic Reactions in Aqueous-Organic Media. XVII. Optical Resoluction of Amino Acid Esters by Enzymatic Hydrolysis in Organic Solvents" Bull. Chem. Soc. Jpn.(1992) 65: 259-2603 (Exhibit 24); and
  • Venter et al., "Synthesis Phenylpropanolamine Derivatives as Potentitial ଲ-Adrenergic Agents" S. Afr. Tydskr. Chem (1978) 31(4): 135-137 (Exhibit 25
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