JAK PI3K/mTOR combination therapy

US9358229B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9358229-B2
Application numberUS-201213571525-A
CountryUS
Kind codeB2
Filing dateAug 10, 2012
Priority dateAug 10, 2011
Publication dateJun 7, 2016
Grant dateJun 7, 2016

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  1. Title

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  2. Abstract

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  5. First independent claim

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.

First claim

Opening claim text (preview).

The invention claimed is: 1. A method of treating primary or idiopathic myelofibrosis, essential thrombocythemia, or polycythemia vera in a subject in need thereof comprising: administering to the subject an effective amount of a combination therapy comprising (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, or a pharmaceutically acceptable salt thereof, wherein the ratio of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile to (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile is from about 3:4 to about 10:1. 2. The method of claim 1 , wherein the subject is human. 3. The method of claim 1 , wherein the compound (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt. 4. The method of claim 1 , wherein (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-pheny]propionitrile, or a pharmaceutically acceptable salt thereof, are in a single formulation or unit dosage form. 5. The method of claim 1 , wherein (3R)-3-cyclopentyl-3[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and 2-methyl-2-[4-(3-methyl-2-oko-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, or a pharmaceutically acceptable salt thereof, are in separate formulitions or unit dosage forms. 6. The method of claim 1 , wherein the treatment comprises administering (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]propionitrile, or a pharmaceutically acceptable salt thereof, at substantially the same time. 7. The method of claim 1 , wherein (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, is administered to the subject, followed by administration of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, or a pharmaceutically acceptable salt thereof. 8. The method of claim 1 , wherein 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, or a pharmaceutically acceptable salt thereof, is administered to the subject, followed by administration of (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof. 9. A method of treating primary myelofibrosis in a subject in need thereof comprising administering to the subject an effective amount of a combination therapy comprising (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, or a pharmaceutically acceptable salt thereof, wherein the ratio of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile to (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile is from about 3:4 to about 10:1.

Assignees

Inventors

Classifications

  • Drugs for disorders of the blood or the extracellular fluid · CPC title

  • specific for leukemia · CPC title

  • condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48) · CPC title

  • Antineoplastic agents · CPC title

  • ortho- or peri-condensed with heterocyclic rings · CPC title

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What does patent US9358229B2 cover?
Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.
Who is the assignee on this patent?
Vannucchi Alessandro M, Bogani Costanza, Bartalucci Niccolo, and 2 more
What technology area does this patent fall under?
Primary CPC classification A61K31/4745. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Jun 07 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).