# US 8,785,470 B2 · Heterocyclic compounds and uses thereof

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- Number: US 8,785,470 B2
- Document ID: US8785470B2
- Status: Granted
- Kind: B2
- Application number: 13/552,516
- Filed: 2012-07-18
- Published: 2013-02-28
- Granted: 2014-07-22
- Earliest claimed: 2011-08-29
- Assignees: Infinity Pharmaceuticals, Inc.
- Applicants: Alfredo C. Castro; Catherine A. Evans; Somarajannair Janardanannair; Andre Lescarbeau; Tao Liu; Daniel A. Snyder; Martin R. Tremblay; Pingda Ren; Yi Liu; Liansheng Li; Katrina Chan
- Inventors: Alfredo C. Castro; Catherine A. Evans; Somarajannair Janardanannair; Andre Lescarbeau; Tao Liu; Daniel A. Snyder; Martin R. Tremblay; Pingda Ren; Yi Liu; Liansheng Li; Katrina Chan
- Web page: https://patentgrep.com/patent/US8785470B2

## CPC

- C07D 401/14: containing three or more hetero rings
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 403/14: containing three or more hetero rings
- C07D 405/14: containing three or more hetero rings
- C07D 411/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 487/04: Ortho-condensed systems
- C07D 495/04: Ortho-condensed systems
- C07D 513/04: Ortho-condensed systems
- C12N 9/1205: {Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases}
- C12Y 207/01137: Phosphatidylinositol 3-kinase (2.7.1.137)
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Y: ENZYMES
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

## Claims

### Claim 1

A compound of the formula:
or a pharmaceutically acceptable form thereof.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the pharmaceutically acceptable form is a pharmaceutically acceptable salt or enantiomer.

### Claim 3

A compound of the formula:

### Claim 4

A compound of the formula:
or a pharmaceutically acceptable form thereof.

### Claim 5 (depends on 4)

The compound of claim 4, wherein the pharmaceutically acceptable form is a pharmaceutically acceptable salt or enantiomer.

### Claim 6

A compound of the formula:

### Claim 7 (depends on 2)

The compound of claim 2, wherein the compound has an (S)-enantiomeric excess of greater than 55%.

### Claim 8 (depends on 2)

The compound of claim 2, wherein the compound has an (S)-enantiomeric excess of greater than 75%.

### Claim 9 (depends on 2)

The compound of claim 2, wherein the compound has an (S)-enantiomeric excess of greater than 90%.

### Claim 10 (depends on 2)

The compound of claim 2, wherein the compound has an (S)-enantiomeric excess of greater than 95%.

### Claim 11 (depends on 2)

The compound of claim 2, wherein the compound has an (S)-enantiomeric excess of greater than 98%.

### Claim 12 (depends on 2)

The compound of claim 2, wherein the compound has an (S)-enantiomeric excess of greater than 99%.

### Claim 13 (depends on 1)

A pharmaceutical composition comprising a compound according to claim 1 and one or more pharmaceutically acceptable excipients.

### Claim 14 (depends on 2)

A pharmaceutical composition comprising a compound according to claim 2 and one or more pharmaceutically acceptable excipients.

### Claim 15 (depends on 3)

A pharmaceutical composition comprising a compound according to claim 3 and one or more pharmaceutically acceptable excipients.

### Claim 16 (depends on 4)

A pharmaceutical composition comprising a compound according to claim 4 and one or more pharmaceutically acceptable excipients.

### Claim 17 (depends on 5)

A pharmaceutical composition comprising a compound according to claim 5 and one or more pharmaceutically acceptable excipients.

### Claim 18 (depends on 6)

A pharmaceutical composition comprising a compound according to claim 6 and one or more pharmaceutically acceptable excipients.

### Claim 19 (depends on 7)

A pharmaceutical composition comprising a compound according to claim 7 and one or more pharmaceutically acceptable excipients.

### Claim 20 (depends on 8)

A pharmaceutical composition comprising a compound according to claim 8 and one or more pharmaceutically acceptable excipients.

### Claim 21 (depends on 9)

A pharmaceutical composition comprising a compound according to claim 9 and one or more pharmaceutically acceptable excipients.

### Claim 22 (depends on 10)

A pharmaceutical composition comprising a compound according to claim 10 and one or more pharmaceutically acceptable excipients.

### Claim 23 (depends on 11)

A pharmaceutical composition comprising a compound according to claim 11 and one or more pharmaceutically acceptable excipients.

### Claim 24 (depends on 12)

A pharmaceutical composition comprising a compound according to claim 12 and one or more pharmaceutically acceptable excipients.
