Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: Novel parenteral and potential oral antithrombotic agents

Journal of Medicinal Chemistry

Volumn 43, Issue 19, 2000, Pages 3453-3473

  Scarborough, R M ^a   Gretler, D D ^a  

^a MILLENNIUM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [[3 [4 (AMINOIMINOMETHYL)PHENYL] 4,5 DIHYDRO 5 ISOXAZOLYL]ACETAMIDO] N [(3,5 DIMETHYL 4 ISOXAZOLYL)SULFONYL]ALANINE; 4 (4 AMIDINOPHENOXY)BUTYRYLASPARTYLVALINE; ABCIXIMAB; ACETYLCYSTEINYLASPARAGINYL 5,5 DIMETHYLTHIOPROLYL 4 AMINOMETHYLPHENYLALANYLGLYCYLASPARTYLCYSTEINE; ANTICOAGULANT AGENT; ARGINYLGLYCYLASPARTYL(O METHYLTYROSINE) AMIDE; CYCLO(DEXTRO 2 AMINOBUTYRYL 2 N METHYLARGINYLGLYCYLASPARTYL 3 AMINOMETHYLBENZOIC ACID) METHANESULFONATE; DISINTEGRIN; FIBRINOGEN RECEPTOR ANTAGONIST; FIBRONECTIN; INTEGRIN; L 734217; L 746 223; LEFRADAFIBAN; LOTRAFIBAN; MK 0852; N [(4 METHYLPHENYL)SULFONYL] 3 [[[5,6,7,8 TETRAHYDRO 4 OXO 5 [2 (4 PIPERIDINYL)ETHYL] 4H PYRAZOLO[1,5 A][1,4]DIAZEPIN 2 YL]CARBONYL]AMINO]ALANINE; N [N [5 [4 (AMINOIMINOMETHYL)PHENYL]PENTANOYL]ASPARTYL]PHENYLALANINE; N [N [5 [4(AMINOMETHYL)PHENYL]PENTANOYL]ASPARTYL]PHENYLALANINE; ORBOFIBAN; RO 435054; ROXIFIBAN; SIBRAFIBAN; SKF 106760; SKF 107260; TRIGRAMIN; UNCLASSIFIED DRUG; XEMILOFIBAN; ZD 2486;

ANGIOPLASTY; CELL ACTIVATION; CELL ADHESION; CELL DIFFERENTIATION; CELL MIGRATION; EXTRACELLULAR MATRIX; IMMUNOGENICITY; LIGAND BINDING; PROTEIN SECONDARY STRUCTURE; REVIEW; STRUCTURE ACTIVITY RELATION; THROMBOCYTE; THROMBOCYTE AGGREGATION; THROMBOSIS;

ADMINISTRATION, ORAL; ANIMALS; ANTIBODIES, MONOCLONAL; CLINICAL TRIALS; DRUG DESIGN; FIBRINOLYTIC AGENTS; HUMANS; INJECTIONS; INTEGRINS; MOLECULAR MIMICRY; PEPTIDES; PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX; SNAKE VENOMS;

EID: 0034699501     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000022w     Document Type: Review

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134. Development of the New Potent Non-Peptide GPIIb/IIIa Antagonist NSL-95301 by Utilizing Combinatorial Technique
135. Development of New Non-peptide GPIIb/IIIa Antagaonists, NSL-95315 and NSL-95317, Isosteres of NSL-95300
136. Antiplatelet Effects of PSA0613, a Newly Developed Oral Non-peptide GP IIb/IIIa Antagonist
137. Discovery of an Orally Active Non-Peptide Fibrinogen Receptor Antagonist
138. Nonpeptide Glycoprotein IIb/IIIa Inhibitors. 19. A New Design Paradigm Employing Linearly Minimized, Centrally Constrained, Exosite Inhibitors
139. Synthesis and Antiplatelet Effects of an Isoxazole Series of Glycoprotein IIb/IIIa Antagonists
140. From Peptide to Non-Peptide. 1. The Elucidation of a Bioactive Conformation of the Arginine-Glycine-Aspartic Acid Recognition Sequence
141. From Peptide to Non-Peptide. 2. The de Novo design of Potent, Non-Peptidal Inhibitors of Platelet Aggregation Based on a Benzodiazepine Scaffold
142. From Peptide to Non-Peptide. 3. Atropisomeric GPIIb-IIIa antagonists Containing the 3,4-Dihydro-1H-1,4-benzodiazepine-2,5-dione Nucleus
143. Preparation and Biological Activity of Novel Tricyclic GPIIb/IIIa Antagonists
144. Direct design of a Potent Non-Peptide Fibrinogen Receptor Antagonist Based on the Structure and Conformation of a Highly Constrained Cyclic RGD Peptide
145. Potent Non-Peptide Fibrinogen Receptor Antagonists Which Present an Alternative Pharmacophore
146. Potent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin Antagonists
147. Lotrafiban
148. Comparison of Inhibition of Platelet Aggregation and GPIIb/IIIa Receptor Occupancy: Evaluation of the Effects of SB 214857, a Low Molecular Weight (LMW) GPIIb/IIIa Receptor Antagonist
149. 3: Evidence for a Common Binding Site for Cyclic Arginyl-Glycinyl-Aspartic Acid Peptides and Nonpeptides
150. The Use of Rabbit Intestinal Permeablility as an In Vitro Assay in the Search for Orally Active GPIIb/IIIa Antagonists
151. Non-Peptide Fibrinogen Receptor Antagonists. 3. Design and Discovery of a Centrally Constrained Inhibitor
152. Non-Peptide Fibrinogen Receptor Antagonists 4. Proposed Three-Dimensional Requirements in Centrally Constrained Inhibitors
153. Nonpeptide GPIIb/IIIa Inhibitors. 10. Centrally Constrained Alpha-Sulfonamides are Potent Inhibitors of Platelet Aggregation
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155. Nonpeptide Glycoprotein IIb/IIIa Inhibitors. 13. Design and Synthesis of an Orally Active Pyrazolopiperazinone Nonpeptide Fibrinogen Receptor Antagonist
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160. Nonpeptide. Glycoprotein IIb/IIIa Inhibitors. 16. Thieno[2,3-b]Thiophene α-Sulfonamides are Potent Inhibitors of Platelet Aggregation
161. Non-Peptide GPIIb/IIIa Inhibitors. 20. Centrally Constrained Thienothiophene α-Sulfonamides Are Potent Long-Acting in Vivo Inhibitors of Platelet Aggregation
162. Nonpeptide Glycoprotein IIb/IIIa Inhibitors. 18. Indole Alpha-Sulfonamide Acids are Potent Inhibitors of Platelet Aggregation
163. Nonpeptide Glycoprotein IIb/IIIa Inhibitors: Substituted Quinazolinediones and Quinazolinones as Potent Fibrinogen Receptor Antagonists
164. Non-Peptide Glycoprotein IIb/IIIa Antagonists. 11. Design and in Vivo Evaluation of 3,4-Dihydro-1(1H)-isoquinolinone-Based Antagonists and Ethyl Ester Prodrugs
165. Design, Synthesis and In Vitro Activities of a Series of Benzimidazole/Benzoxazole Glycoprotein IIb/IIIa Inhibitors
166. Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists
167. Fibrinogen Receptor (GPIIb-IIIa) Antagonists Derived from 5,6-Bicyclic Templates. Amidinoindoles, Amidinoindazoles, and Amidinobenzofurans Containing the N-α-Sulfonamide Carboxylic Acid Function as Potent Platelet Aggregation Inhlbitors
168. Non-Peptide RGD Surrogates Which Mimic a Gly-Asp β-Turn: Potent Antagonists of Platelet Glycoproteln IIb-IIIa
169. Dihydroisoquinolone RGD Mimics. Exploration of the Aspartate Isostere
170. Fused Bicyclic Gly-Asp β-Turn Mimics With Specific Affinity for GPIIb-IIIa
171. New Platelet Fibrinogen Receptor Glycoprotein IIb-IIIa Antagonists: Orally Active Series of N-Alkylated Amidines with a 6,6-Bicyclic Template
172. Antiaggregatory, Antithrombotic Effects of MS-180, a Novel Platelet Glycoprotein IIb/IIIa Receptor Antagonist
173. Pharmacokinetics and Pharmacodynamics of Sibrafiban, an Orally Administered IIb/IIIa Antagonist, in Patients with Acute Coronary Syndrome
174. Pharmacokinetic and Pharmacodynamics of Ro 44-3888 After Single Ascending Oral Doses of Sibrafiban, an Oral Platelet Aggregation Inhibitor, in Healthy Male Volunteers
175. Fibrinogen Receptor Antagonist-Induced Thrombocytopenia in Chimpanzee and Rhesus Monkey Associated with Preexisting Drug-Dependent Antibodies to Platelet Glycoprotein IIb/IIIa
176. Platelet Activation as a Potential Mechanism of GP IIb/IIIa Inhibitor-Induced Thrombocytopenia
177. Pharmacodynamic Efficiacy, Clinical Safety, and Outcomes After Prolonged Platelet Glycoprotein IIb/ IIIa Receptor Blockade with Oral Xemilofiban: Results of a Multicenter, Placebo-controlled, Randomized Trial
178. Meeting Highlights. Highlights of the 48(th) Scientific Session of the American College of Cardiology
179. Long-term Oral Platelet Glycoprotein IIb/IIIa Receptor Antagonism with Sibrafiban After Acute Coronary Syndromes: Study Design of the Sibrafiban Versus Aspirin to Yield Maximum Protection from Ischemic Heart Events Post-acute Coronary Syndromes (SYMPHONY) Trial
180. Comparison of Sibrafiban with Aspirin for Prevention of Cardiovascular Events After Acute Coronary Syndromes: A Randomized Trial
181. Induction of Fibrinogen Binding and Platelet Aggregation as a Potential Intrinsic Property of Various GPIIb/IIIa (αIIb/β3) Inhibitors
182. 2+ Signaling
183. Increased Mortality With Oral Glycoprotein IIb/IIIa Antagonists: A Pooled Analysis of the Large Scale Oral Glycoprotein IIb/IIIa Trials
184. Increase Platelet Reactivity in Patients Given Orbofiban After an Acute Coronary Syndrome: An OPUS-TIMI 16 Substudy
185. Randomized Trial of an Oral Platelet Glycoprotein IIb/IIIa Antagonist, Sibrafiban, in Patients after an Acute Coronary Syndrome: Results of the TIMI 12 Trial
186. Second Generation Oral IIb/IIIa Receptor Blockade: Phase II Experience With Roxifiban
187. Dose-finding and Tolerability of a New Oral Platelet Glycoprotein IIb/IIIa Inhibitor, SB 214857, in Patients with Coronary Artery and Cerebrovascular Disease: The APLAUD Results
188. Design of the Blockage of the Glycoprotein IIb/IIIa Receptor to Avoid Vascular Occlusion (BRAVO) Trial
189. Long-term Treatment With a Platelet Glycoprotein-Receptor Antagonist After Percutaneous Coronary Revascularization
190. Oral Glycoprotein IIb/IIIa Inhibition with Orbofiban in Patients With Unstable Coronary Syndromes
191. Oral Glycoprotein IIb/IIIa Inhibition with Orbofiban in Patients With Unstable Coronary Syndromes (OPUS-TIMI 16) Trial
192. Results From Late-Breaking Clinical Trials Sessions at ACCIS 2000 and ACC 2000
193. Reduction in Atherosclerotic Lesion Size in Pigs by αvβ3 Inhibitors is Associated With Inhibition of Insulin-Like Growth Factor-I-Mediated Signaling
194. Design and Characterization of Orally Active Arg-Gly-Asp Peptidomimetic Vitronectin Receptor Antagonist SB 265123 for Prevention of Bone Loss in Osteoporosis
195. Selective, Tight-binding Inhibitors of Integrin alpha4 beta1 that Inhibit Allergic Airway Responses
196. Folding of the N-Terminal, Ligand-binding Region of Integrin α-Subunits into a β-Propeller Domain
197. Signal Transduction Pathways for Mouse Platelet Membrane Adhesion Receptors
198. 3-(GPIIb-IIIa) Tyrosine Phosphorylation Induced by Platelet Aggregation
199. 3 Signaling and Platelet Function
200. Strategies Toward the Design of Novel and Selective Protein Tyrosine Kinase Inhibitors
201. Protein Tyrosine Kinase Inhibitors as Novel Therapeutic Agents
202. Rapid Platelet-Function Assay. An Automated and Quantitative Cartridge-Based Method