Processes for preparing amine salts of sildenafil-analogues and use thereof

• US 8,497,370 B2
• Filed: 03/10/2011
• Issued: 07/30/2013
• Est. Priority Date: 11/02/2010
• Status: Active Grant

• Current Assignee: Kaohsiung Medical University
• Original Assignee: Kaohsiung Medical University
• Inventors: Chen, Ing-Jun
• Primary Examiner(s): Gembeh, Shirley V
• Application Number:
  US13/044,899
• Publication Number:
  US 20120108604A1
• Time in Patent Office: 873 Days
• Field of Search: 514/252.16, 544/270, 536/31
• US Class Current: 544/270
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 17/14 for baldness or alopecia
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/12 Antihypertensives
• CPC Class Codes: C07D 487/04 Ortho-condensed systems
• CPC Class Codes: C08L 1/286 substituted with acid radicals, e.g. carboxymethyl cellulose [CMC] C08L1/282 takes precedence
• CPC Class Codes: C08L 5/00 Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00

Abstract

A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R₁, R_a and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.

Claims

1. A complex salt, comprising a structure of

2. A complex salt as claimed in claim 1, wherein RX is a Statin derivative being one selected from a group consisting of Atorvastatin, Cerivastatin, Fluvastatin, Lovastatin, Mevastatin, Pravastatin, Rosuvastatin and Simvastatin.

3. A complex salt as claimed in claim 1, wherein RX is the γ

-polyglutamic acid derivative being one selected from a group consisting of an alginate sodium, a γ

-polyglutamic acid, a sodium polyglutamate, a GLT and a calcium polyglutamate-alginate sodium.

4. A pharmaceutical composition, comprising:

an effective amount of a complex salt of

5. A pharmaceutical composition as claimed in claim 4, wherein the Statin derivative is one selected from a group consisting of Atorvastatin, Cerivastatin, Fluvastatin, Lovastatin, Mevastatin, Pravastatin, Rosuvastatin and Simvastatin.

6. A pharmaceutical composition as claimed in claim 4, wherein the γ

-polyglutamic acid derivative is one selected from a group consisting of an alginate sodium, a γ

-polyglutamic acid, a sodium polyglutamate, a GLT, a calcium polyglutamate-alginate sodium.

7. A pharmaceutical composition as claimed in claim 4, wherein the complex salt is a Sildenafil-analogue being one of Acetidenafil, and Vardenafil.

8. A pharmaceutical composition comprising:

9. A pharmaceutical composition as claimed in claim 8, wherein the Statin derivative is one selected from a group consisting of Atorvastatin, Cerivastatin, Fluvastatin, Lovastatin, Mevastatin, Pravastatin, Rosuvastatin and Simvastatin.

10. A pharmaceutical composition as claimed in claim 8, wherein the γ

-polyglutamic acid derivative is one selected from a group consisting of an alginate sodium, a γ

-polyglutamic acid, a sodium polyglutamate, a GLT and a calcium polyglutamate-alginate sodium.