N-[ (R) -1-{3- (4- piperidyl) propionyl } -3-piperidylcarbonyl] -2 (S) -acetylamino-beta -alanine as fibrinogen receptor antagonist

• US 20010016571A1
• Filed: 03/15/2001
• Published: 08/23/2001
• Est. Priority Date: 03/13/1996
• Status: Abandoned Application

• Current Assignee: Fujisawa Pharmaceutical Co., Ltd. (Astellas Pharma Incorporated)
• Original Assignee: Fujisawa Pharmaceutical Co., Ltd. (Astellas Pharma Incorporated)
• Inventors: Ohkubo, Mitsuru, Yamanaka, Toshio, Takahashi, Fumie, Kato, Masayuki
• Application Number:
  US09/805,996
• Publication Number:
  US 20010016571A1
• Time in Patent Office: Days
• US Class Current: 514/19
• CPC Class Codes: C07D 211/60 Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

This invention relates to β-alanine derivative represented by the following formula (I);

which is glycoprotein IIB/IIla antagonist, inhibitor of blood platelets aggregation and inhibitor of the binding of fibrinogen to blood platelets, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Claims

1. A compound of the formula (I):

2. A process for preparing a compound of

claim 1

, which comprises

(i) subjecting a compound of the formula:

wherein R¹ is amino protective group, or a salt thereof, to elimination reaction of the amino protective group, to give a compound of the formula;

(ii) subjecting a salt of a compound of the formula;

to desalting reaction, to give a compound of the formula;

3. A pharmaceutical composition which comprises, as an active ingredient, a compound of

claim 1

in admixture with pharmaceutically acceptable carriers or excipients.

4. Use of a compound of

claim 1

for the manufacture of a medicament.

5. A compound of

claim 1

for use as a medicament.

6. A method for the prevention and/or the treatment of diseases caused by thrombus formation;

estenosis or reocclusion;

the thrombus formation in case of vascular surgery, valve replacement, extracorporeal circulation or transplantation;

disseminated intravascular coagulation;

thrombotic thrombocytopenic;

essential thrombocytosis;

inflammation;

immune diseases;

or metastasis;

or for the adjuvant therapy with thrombolytic drug or anticoagulant;

which comprises administering a compound of

claim 1

to a human being or an animal.