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733 results about "Protein kinase inhibitor" patented technology

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A protein kinase inhibitor is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that add a phosphate (PO₄) group to a protein, and can modulate its function.

AKT protein kinase inhibitors

InactiveUS20050130954A1BiocideOrganic chemistryPTK InhibitorsEnantiomer

The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

AKT protein kinase inhibitors

AKT protein kinase inhibitors

AKT protein kinase inhibitors

Owner:ARRAY BIOPHARMA

6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors

ActiveUS20060235031A1Treatment and/or prevention of hyperproliferative diseasesBiocideSenses disorderDiseasePTK Inhibitors

Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and / or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy / asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors

6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors

6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors

Owner:ACERTA PHARMA BV

Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors

InactiveUS7098330B2BiocideNervous disorderArylPTK Inhibitors

This invention describes novel pyrazole compounds of formula III:wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors

Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors

Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors

InactiveUS7008948B2BiocideNervous disorderArylPTK Inhibitors

This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors

Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors

Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Compositions useful as inhibitors of protein kinases

InactiveUS20050148603A1Effective inhibitorAvoid cell deathOrganic active ingredientsBiocideDiseaseBiochemistry

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Owner:VERTEX PHARMA INC

Pyrazole compounds useful as protein kinase inhibitors

InactiveUS6989385B2BiocideSenses disorderArylPTK Inhibitors

This invention describes novel pyrazole compounds of formula IIc: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors

InactiveUS20100048540A1Impart oxidative damage to surrounding DNAInhibitory activityBiocideOrganic chemistryPTK InhibitorsBiochemistry

The invention relates to novel heterocyclic N-oxides which are useful as hypoxic selective cytotoxic agents that mediate and / or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted ahgiogenesis and / or cellular proliferation by administering effective amounts of such compounds.

Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors

Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors

Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors

Owner:SENTINEL ONCOLOGY

Pyrazolopyrimidines as protein kinase inhibitors

InactiveUS20060094706A1Reduce usageUseful in treatmentBiocideSteroidsDiseasePTK Inhibitors

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and / or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

Pyrazolopyrimidines as protein kinase inhibitors

Pyrazolopyrimidines as protein kinase inhibitors

Pyrazolopyrimidines as protein kinase inhibitors

Owner:MERCK SHARP & DOHME LLC

Compositions useful as inhibitors of protein kinases

InactiveUS20050137201A1BiocideNervous disorderBiochemistryDisease cause

The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Owner:VERTEX PHARMA INC

Compositions useful as inhibitors of protein kinases

InactiveUS6846928B2Avoid cell deathTreat and prevent reperfusion/ischemiaBiocideOrganic chemistryDiseasePTK Inhibitors

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Owner:VERTEX PHARMA INC

Protein Kinase Inhibitors

InactiveUS20090143399A1Inhibits protein kinase activityOrganic active ingredientsOrganic chemistryDiseasePTK Inhibitors

Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure:including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from:and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Protein Kinase Inhibitors

Protein Kinase Inhibitors

Protein Kinase Inhibitors

Owner:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA +1

Compositions useful as inhibitors of protein kinases

InactiveUS7091343B2Avoid cell deathTreat and prevent reperfusion/ischemiaBiocideOrganic chemistryDiseaseProtein kinase domain

The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Owner:VERTEX PHARMA INC

Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors

ActiveUS7750007B2Inhibitory activityBiocideOrganic chemistryProtein kinase inhibitor activityPTK Inhibitors

The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II):or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.

Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors

Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors

Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors

Owner:SUMITOMO PHARMA ONCOLOGY INC

4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors

InactiveUS6610688B2BiocideOrganic active ingredientsDiseasePTK Inhibitors

This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and / or prevention of diseases such as, but not limited to, cancer.

4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors

4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors

4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors

Owner:SUGEN INC

Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases

InactiveUS20060135537A1Effective inhibitorBiocideOrganic active ingredientsDiseasePyrazole

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention.

Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases

Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases

Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases

Owner:VERTEX PHARMA INC

Indazole compounds useful as protein kinase inhibitors

InactiveUS7041687B2Reduce severityBiocideNervous disorderPTK InhibitorsTyrosine-kinase inhibitor

The present invention provides compounds of formula I:or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.

Indazole compounds useful as protein kinase inhibitors

Indazole compounds useful as protein kinase inhibitors

Indazole compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Compositions useful as inhibitors of protein kinases

InactiveUS7179826B2Avoid cell deathTreat and prevent reperfusion/ischemiaBiocideOrganic chemistryDiseaseProtein kinase domain

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Compositions useful as inhibitors of protein kinases

Owner:VERTEX PHARMA INC

Heterocyclic inhibitors of ERK2 and uses thereof

InactiveUS7253187B2Antibacterial agentsBiocideDiabetes mellitusPTK Inhibitors

Described herein are compounds that are useful as protein kinase inhibitors having the formula:wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

Heterocyclic inhibitors of ERK2 and uses thereof

Heterocyclic inhibitors of ERK2 and uses thereof

Heterocyclic inhibitors of ERK2 and uses thereof

Owner:VERTEX PHARMA INC

Compounds useful as inhibitors of atr kinase

InactiveUS20120046295A1Surprising synergyInhibitor usedBiocideOrganic chemistryKinase inhibitionPyrrole

The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.

Compounds useful as inhibitors of atr kinase

Compounds useful as inhibitors of atr kinase

Compounds useful as inhibitors of atr kinase

Owner:VERTEX PHARMA INC

Heterocyclic inhibitors of ERK2 and uses thereof

InactiveUS20050234059A1BiocideOrganic chemistryPTK InhibitorsMedicine

Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

Heterocyclic inhibitors of ERK2 and uses thereof

Heterocyclic inhibitors of ERK2 and uses thereof

Heterocyclic inhibitors of ERK2 and uses thereof

Owner:VERTEX PHARMA INC

Pyrazole compounds useful as protein kinase inhibitors

InactiveUS7691853B2Organic active ingredientsBiocideDiseasePTK Inhibitors

This invention describes novel pyrazole compounds of formula IV:wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Aminopyrimidines useful as kinase inhibitors

InactiveUS20070179125A1Inhibitor usedBiocideOrganic active ingredientsKinase inhibitionDisease cause

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.

Aminopyrimidines useful as kinase inhibitors

Aminopyrimidines useful as kinase inhibitors

Aminopyrimidines useful as kinase inhibitors

Owner:VERTEX PHARMA INC

Pyrazole compounds useful as protein kinase inhibitors

InactiveUS20050004110A1BiocideNervous disorderDiseaseAryl

This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered carbocyclo ring; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Protein kinase inhibitors

InactiveUS20050227992A1Organic active ingredientsOrganic chemistryDiseasePTK Inhibitors

Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Protein kinase inhibitors

Protein kinase inhibitors

Protein kinase inhibitors

Owner:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA

Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

ActiveUS7354939B2BiocideNervous disorderDiseaseCombinatorial chemistry

The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

Owner:VERTEX PHARMA INC

Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors

ActiveUS20100004239A1BiocideSenses disorderPTK InhibitorsTyrosine-kinase inhibitor

The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).

Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors

Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors

Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors

Owner:SHANGHAI HENGRUI PHARM CO LTD

Heterocyclic inhibitors of ERK2 and uses thereof

InactiveUS7304061B2BiocideOrganic chemistryPTK InhibitorsMedicine

Described herein are compounds that are useful as protein kinase inhibitors having the formula:wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

Heterocyclic inhibitors of ERK2 and uses thereof

Heterocyclic inhibitors of ERK2 and uses thereof

Heterocyclic inhibitors of ERK2 and uses thereof

Owner:VERTEX PHARMA INC

Pyrazole compositions useful as inhibitors of ERK

InactiveUS6949580B2BiocideNervous disorderPTK InhibitorsMammal

Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Pyrazole compositions useful as inhibitors of ERK

Pyrazole compositions useful as inhibitors of ERK

Pyrazole compositions useful as inhibitors of ERK

Owner:VERTEX PHARMA INC

Bicyclic protein kinase inhibitors

InactiveUS20070149521A1BiocideOrganic chemistryPTK InhibitorsDisease cause

Compounds of the Formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit protein kinase enzymes and are useful for the treatment and / or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy / asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

Bicyclic protein kinase inhibitors

Bicyclic protein kinase inhibitors

Bicyclic protein kinase inhibitors

Owner:OSI PHARMA INC

Pyrazole compositions useful as inhibitors of erk

InactiveUS7056944B2BiocideNervous disorderPTK InhibitorsMammal

Described herein are compounds that are useful as protein kinase inhibitors having the formula:where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Pyrazole compositions useful as inhibitors of erk

Pyrazole compositions useful as inhibitors of erk

Pyrazole compositions useful as inhibitors of erk

Owner:VERTEX PHARMA INC

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