Stable polymorph of N-(3-ethynylphenyl)-6, 7-bis (2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

US 20050090500A1
Filed: 11/18/2004
Published: 04/28/2005
Est. Priority Date: 11/11/1999
Status: Active Grant

First Claim

Patent Images

1-54. -54. (canceled)

View all claims

1 Assignment

Timeline View

Assignment View

0 Petitions

Accused Products

Abstract

The present invention relates to a stable crystalline form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride designated the B polymorph, its production in essentially pure form, and its use. The invention also relates to the pharmaceutical compositions containing the stable polymorph B form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride, as well other forms of the compound, and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.

36 Citations

View as Search Results

69 Claims

1-54. -54. (canceled)

55. A method of monotherapy for a subject suffering from abnormal cell growth expressing the epidermal growth factor receptor (EGFR) which comprises orally administering to the subject a therapeutically effective amount of a crystalline polymorph of the hydrochloride salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine so as to treat the subject.
- View Dependent Claims (56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69)
- - 56. The method of claim 55, wherein the abnormal cell growth is brain cancer, squamous cell cancer, bladder cancer, gastric cancer, pancreatic cancer, hepatic cancer, glioblastoma multiforme breast cancer, head cancer, neck cancer, esophageal cancer, prostate cancer, colorectal cancer, lung cancer, renal cancer, kidney cancer, ovarian cancer, gynecological cancer, thyroid cancer, non-small cell lung cancer (NSCLC), refractory ovarian cancer, or head and neck cancer.
  - 57. The method of claim 55, wherein the abnormal cell growth is non-small cell lung cancer (NSCLC).
  - 58. The method of claim 55, wherein the abnormal cell growth is refractory ovarian cancer.
  - 59. The method of claim 55, wherein the abnormal cell growth is head and neck cancer.
  - 60. The method of claim 55, wherein the therapeutically effective amount is from about 0.001 to about 100 mg/kg/day.
  - 61. The method of claim 55, wherein the therapeutically effective amount is from about 1 to about 35 mg/kg/day.
  - 62. The method of claim 55, wherein the therapeutically effective amount is from about 1 to about 7000 mg/day.
  - 63. The method of claim 55, wherein the therapeutically effective amount is from about 5 to about 2500 mg/day.
  - 64. The method of claim 55, wherein the therapeutically effective amount is from about 5 to about 200 mg/day.
  - 65. The method of claim 55, wherein the therapeutically effective amount is from about 25 to about 200 mg/day.
  - 66. The method of claim 55, wherein the treatment is a palliative or neo-adjuvant/adjuvant monotherapy.
  - 67. The method of claim 55, wherein the EGFR receptor is the EGFRvIII receptor.
  - 68. The method of claim 55, wherein the therapeutically effective amount is from 100 to 1600 mg/week.
  - 69. The method of claim 55, wherein the therapeutically effective amount is orally administered weekly.

Specification

Resources

Litigation Campaign Assessment

Current Assignee
OSI Pharmaceuticals LLC (Astellas Pharma Incorporated)
Original Assignee
Osi Pharmaceuticals Incorporated (Astellas Pharma Incorporated)
Inventors
Moyer, James D., Norris, Timothy, Raggon, Jeffrey W., Morin, Michael J., Foster, Barbara A., Ferrante, Karen J., Kajiji, Shama M., Silberman, Sandra L., Connell, Richard D.

Granted Patent

US 7,087,613 B2
Time in Patent Office

Days
Field of Search
US Class Current

514/249
CPC Class Codes

A61K 2300/00   Mixtures or combinations of...

A61K 31/517   ortho- or peri-condensed wi...

A61K 45/06   Mixtures of active ingredie...

A61P 35/00   Antineoplastic agents

C07D 239/94   Nitrogen atoms

Stable polymorph of N-(3-ethynylphenyl)-6, 7-bis (2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

First Claim

1 Assignment

0 Petitions

Accused Products

Abstract

36 Citations

69 Claims

Specification

Solutions

Use Cases

Quick Links

Stable polymorph of N-(3-ethynylphenyl)-6, 7-bis (2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

First Claim

1 Assignment

Subscription Required

Subscription Required

0 Petitions

Subscription Required

Accused Products

Subscription Required

Abstract

36 Citations

69 Claims

Specification

Subscription Required

Solutions

Use Cases

Quick Links