Fadila Derguini

US Patent:

55212212, May 28, 1996

Filed:

Apr 9, 1991

Appl. No.:

7/682909

Inventors:

Jochen Buck - New York NY
Ulrich Hammerling - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY
The Trustees of Columbia University in the City of New York - New York NY

International Classification:

C07C 3518
C07C 3768

US Classification:

514725

Abstract:

This invention provides a purified retro-retinoid compound characterized by a molecular mass of about 302 daltons. Also provided by this invention is a method of enhancing the growth of a cell in a vitamin A reduced environment which comprises contacting the cell with an effective growth enhancing amount of a compound having a structure: ##STR1## wherein the configuration of the C6, C8, C10 and C12 double bond independently is Z or E and the absolute configuration at C-14 is independently R or S; wherein R. sub. 1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acid halide, amide, nitrile, or amine; and wherein R. sub. 2 is hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R. sub. 1 and R. sub. 2 are replaced by a 14, 15-oxirane group; and wherein the retro structure is alpha or gamma. Further provided are a method for enhancing transcription of a gene regulated by retinoid in a cell, or a method for enhancing an immune response in a subject.

US Patent:

61504211, Nov 21, 2000

Filed:

Jun 2, 1998

Appl. No.:

9/088770

Inventors:

Lorraine Gudas - New York NY
Fadila Derguini - New York NY

Assignee:

Cornell Research Foundation, Inc. - Ithaca NY

International Classification:

A61K 3112
A61K 3111

US Classification:

514690

Abstract:

Certain retinoids with CH. sub. 2 OH at the side chain terminal position, preferably 4-oxoretinol, inhibit growth of estrogen-receptor positive and estrogen-receptor negative breast cancer tumor cell lines and have utility for adjuvant therapy and treatment of metastatic disease.

US Patent:

58831363, Mar 16, 1999

Filed:

Jun 7, 1995

Appl. No.:

8/478411

Inventors:

Ulrich Hammerling - New York NY
Jochen Buck - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY
The Trustees of Columbia University in the City of New York - New York NY

International Classification:

A61K 31015
A61K 3107

US Classification:

514763

Abstract:

This invention provides methods of inhibiting the growth of cells, of treating a subject having a disease characterized by an uncontrolled growth of cells and of blocking an immune response as well as related inflammatory responses in a subject which comprises administering a compound having the structure: ##STR1##.

US Patent:

56485638, Jul 15, 1997

Filed:

Jun 7, 1995

Appl. No.:

8/481913

Inventors:

Jochen Buck - New York NY
Ulrich Hammerling - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY
The Trustees of Columbia University in the City of New York - New York NY

International Classification:

C07C 3518
C07C 3768

US Classification:

568824

Abstract:

This invention provides a homogeneous retro-retinoid compound, a method of enhancing the growth of a cell in a vitamin A reduced environment, a method for enhancing transcription of a gene regulated by retinoid in a cell, and a method for enhancing an immune response in a subject, wherein the compound has the structure: ##STR1##.

US Patent:

59625341, Oct 5, 1999

Filed:

Jul 3, 1997

Appl. No.:

8/887633

Inventors:

Lorraine J. Gudas - New York NY
Charles Achkar - North Bergen NJ
Jochen Buck - New York NY
Alexander W. Langston - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Cornell Research Foundation, Inc. - Ithaca NY

International Classification:

A61K 3112
A61K 3111

US Classification:

514690

Abstract:

For the first time, certain retinoids with a side chain terminal CH. sub. 2 OH group or ester or ether thereof or aldehyde rather than a side chain terminal COOH group and substitution at the 4-position have been indicated to bind to nuclear receptors and to be biologically active in inducing cell differentiation of normal and tumor cells. These compounds activate gene expression through binding to nuclear receptor proteins. These compounds induce differentiation in normal and cancer cells and are useful for treating leukemias, and lymphomas, squamous cell carcinomas, deep (cystic) acne, psoriasis and photodamaged or aging skin. These compounds have stability and in vitro half-life advantages over and solubility differences from all-trans-retinoic acid and activity advantages over 13-cis retinoic acid.

US Patent:

56102003, Mar 11, 1997

Filed:

Apr 10, 1995

Appl. No.:

8/420435

Inventors:

Ulrich Hammerling - New York NY
Jochen Buck - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY
The Trustees of Columbia University in the City of New York - New York NY

International Classification:

A61K 31015
A61K 3107

US Classification:

514763

Abstract:

This invention provides methods of inhibiting the growth of cells, of treating a subject having a disease characterized by an uncontrolled growth of cells and of blocking an immune response as well as related inflammatory responses in a subject which comprises administering a compound having the structure: ##STR1##.

US Patent:

57863911, Jul 28, 1998

Filed:

Jan 11, 1995

Appl. No.:

8/371535

Inventors:

Lorraine J. Gudas - New York NY
Charles Achkar - North Bergen NJ
Jochen Buck - New York NY
Alexander W. Langston - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Cornell Research Foundation, Inc. - Ithaca NY
The Trustees of Columbia University in the City of New York - New York NY

International Classification:

A61K 31115
A61K 31045
A61K 3108

US Classification:

514690

Abstract:

For the first time, certain retinoids with a side chain terminal CH. sub. 2 OH group or ester or ether thereof or aldehyde rather than a side chain terminal COOH group and substitution at the 4-position have been indicated to bind to nuclear receptors and to be biologically active in inducing cell differentiation of normal and tumor cells. These compounds activate gene expression through binding to nuclear receptor proteins. These compounds induce differentiation in normal and cancer cells and are useful for treating leukemias, and lymphomas, squamous cell carcinomas, deep (cystic) acne, psoriasis and photodamaged or aging skin. These compounds have stability and in vitro half-life advantages over and solubility differences from all-trans-retinoic acid and activity advantages over 13-cis retinoic acid.

US Patent:

59088680, Jun 1, 1999

Filed:

Jun 5, 1995

Appl. No.:

8/331627

Inventors:

Jochen Buck - New York NY
Ulrich Hammerling - New York NY
Fadila Derguini - New York NY
Koji Nakanishi - New York NY

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY

International Classification:

A61K 31045
A61K 3107
A61K 31075

US Classification:

514725

Abstract:

The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C. sub. 20 H. sub. 32 O. sub. 3. The present invention also provides a purified retinoid compound having the following structure: ##STR1## wherein the configuration of C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is hydroxyl, alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; wherein R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively. Also provided by this invention is a pharmaceutical composition which comprises the compound above and a pharmaceutically acceptable carrier. This invention further provides a growth medium comprising the compound above at a concentration effective to enhance cell growth.