The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: [structure] Also provided in the present invention are methods of using such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.

Claims

31 · 2 independent · depth 7

31 granted claims

›1.independentAn isolated compound of Formula II-A-1:+28

›2.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, whereinnR1 is -L-C1-10alkyl, -L-C3-8cycloalkyl, -L-C1-10alkylheterocylyl,…d2

›3.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, wherein â€”W2â€” is â€”NRâ€²â€”, â€”N(R7)C(O)â€” or â€”N(R7)S(O)2â€”, and…d2

›4.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, wherein R2 is H.d2

›5.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, wherein:nR1 is -L-C1-10alkyl or -L-C3-8cycloalkyl, each of which is unsub…d2

›6.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, wherein R31 and R32 are each H.d2

›7.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, wherein the compound inhibits mammlian target of rapamycin (mTOR) at an I…d2

›8.↳ 1A composition comprising a compound or pharmaceutically acceptable salt of claim 1, and a pharmaceutically acceptable carrier.d2+4

›13.↳ 1The compound or pharmaceutically acceptable salt of the compound of claim 1, wherein the compound is:d2+14

›16.↳ 13multiple · 13, 14, 15A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt of any one of claim 13, 14 or 15, and further comprising a ph…d3+13

›17.↳ 16The pharmaceutical composition of claim 16, wherein the compound or pharmaceutically acceptable salt is in a therapeutically effective amount.d4+6

›24.↳ 16The pharmaceutical composition of claim 16, wherein the pharmaceutical excipient is chosen from the group consisting of detackifiers, anti-foaming age…d4

›25.↳ 16The pharmaceutical composition of claim 16, wherein the pharmaceutical composition is a formulation for oral administration.d4

›26.↳ 16The pharmaceutical composition of claim 16, wherein the pharmaceutical composition is a solid dosage form.d4+2

›29.↳ 16The pharmaceutical composition of claim 16, wherein the pharmaceutical composition is a liquid dosage form.d4

›30.↳ 1The compound or pharmaceutically acceptable salt of claim 1, wherein the compound or pharmaceutically acceptable salt inhibits mTor at an IC50 value o…d2

›31.↳ 1The compound or pharmaceutically acceptable salt of claim 1, wherein the compound or pharmaceutically acceptable salt inhibits mTor at an IC50 value o…d2

›14.independentAn isolated compound of Formula:+1

Classifications

9 codes

IPC · International Patent Classification

Section A — Human necessities

A61P9/00
A61P35/00
A61P29/00
A61K31/519

Section C — Chemistry; metallurgy

C07D487/04

USPC · US Patent Classification

514/262.1514/265.1544/280544/262

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Pendency

3.7 y

1,349 days filing → grant

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after a restriction

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Examiner

Susanna Moore

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Priority chain

2 priority documents

Priority

3 Nov 2008

earliest claimed

›Priority documents — 2

Type	Document	Date
provisional	US 61198200	3 Nov 2008
related publication	US 20100184760 A1	22 Jul 2010

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