Sak Halekoe Khammungkhune

US Patent:

6372739, Apr 16, 2002

Filed:

Jul 2, 2001

Appl. No.:

09/897048

Inventors:

Bernd M. Stein - San Diego CA
David Wesley Anderson - Poway CA
Mary Doubleday - Doylestown PA
Graziella I. Shevlin - San Diego CA
Adam Kois - San Diego CA
Sak Khammungkhune - San Diego CA
Ravi Kumar Jalluri - San Diego CA
Shripad S. Bhagwat - San Diego CA
Jeffrey A. McKie - San Diego CA

Assignee:

Signal Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 315377

US Classification:

5142335, 544151, 546187, 546193, 546196, 5483114, 548525, 549289

Abstract:

Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: wherein R , R , R , n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.

US Patent:

20070276139, Nov 29, 2007

Filed:

Feb 10, 2005

Appl. No.:

10/597808

Inventors:

Quanlai Song - Carlsbad CA, US
Sak Khammungkhune - San Diego CA, US
Bruce Ross - Carlsbad CA, US
Richard Griffey - Vista CA, US

International Classification:

C07D 311/82
C07D 335/12
C07H 19/06
C07H 21/00

US Classification:

544243000, 544317000, 549223000, 549027000

Abstract:

The present invention describes an improved hydroxyl protecting group of formula (1), wherein Rand Rare specified substituents and Q is O, S, NRor N(C═O)R.

US Patent:

62914561, Sep 18, 2001

Filed:

Jan 27, 2000

Appl. No.:

9/492939

Inventors:

Bernd M. Stein - San Diego CA
David Wesley Anderson - Poway CA
May S. Sutherland - Bothell WA
Mary Doubleday - Doylestown PA
Graziella I. Shevlin - San Diego CA
Adam Kois - San Diego CA
Sak Khammungkhune - San Diego CA
Ravi Kumar Jalluri - San Diego CA
Shripad S. Bhagwat - San Diego CA
Jeffrey A. McKie - San Diego CA

Assignee:

Signal Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 315377
A61P 1908
C07D41312

US Classification:

5142335

Abstract:

Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: ##STR1## wherein R. sub. 1, R. sub. 2, R. sub. 3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.

US Patent:

63315629, Dec 18, 2001

Filed:

Jul 6, 2000

Appl. No.:

9/611156

Inventors:

Shripad S. Bhagwat - San Diego CA
Jeffrey A. McKie - San Diego CA
Sak Khammungkhune - San Diego CA

Assignee:

Signal Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 3137
A61P 3500
C07D31112

US Classification:

514457

Abstract:

Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: ##STR1## wherein R. sub. 1, R. sub. 2, R. sub. 3, n and p are as defined here. In a specific embodiment, the compounds are selective modulators for Er-. beta. over ER-. alpha. Methods are also disclosed for modulating ER-. beta. in cells and/or tissues expressing the same, including cells and/or tissues that preferentially express ER-. beta. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.