John A Katzenellenbogen

US Patent:

20030119800, Jun 26, 2003

Filed:

Jun 7, 2002

Appl. No.:

10/165380

Inventors:

Stavros Manolagas - Little Rock AR, US
John Katzenellenbogen - Urbana IL, US

International Classification:

A61K031/56

US Classification:

514/178000, 514/182000

Abstract:

A variety of bone anabolic compounds are useful for maintaining and/or increasing bone mass, density, and/or strength in mammals. Preferred compounds enhance bone anabolic activity while minimizing or eliminating undesirable feminizing or masculinizing effects.

US Patent:

20070021495, Jan 25, 2007

Filed:

Jul 25, 2006

Appl. No.:

11/459917

Inventors:

John Katzenellenbogen - Urbana IL, US
Benita Katzenellenbogen - Urbana IL, US
Dennis Compton - Champaign IL, US

International Classification:

A61K 31/381
A61K 31/34
A61K 31/195
A61K 31/18
C07D 333/32
C07D 307/02
C07C 303/00

US Classification:

514445000, 514471000, 514602000, 514562000, 549065000, 549475000, 564086000

Abstract:

Compounds, pharmaceutically acceptable salts, stereoisomers and prodrugs thereof, that are ER ligands and particularly to such compounds that are ER beta-selective and/or ER beta-specific ligands. Compounds herein include certain compounds which are ER beta-selective agonists. Compounds herein include ER beta-selective agonists which exhibit minimal agonist or antagonist effect on ER alpha. Compounds of the invention include those of formula I: and any pharmaceutically acceptable salts, stereoisomers and prodrugs thereof wherein AR, R, R, and X—Xare as defined hereinabove.

US Patent:

20120052570, Mar 1, 2012

Filed:

Jan 22, 2010

Appl. No.:

13/145752

Inventors:

Daniel Metzger - Strasbourg, FR
Pierre Chambon - Blaesheim, FR
Huimin Zhao - Champaign IL, US
John Katzenellenbogen - Urbana IL, US

Assignee:

CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - Paris
UNIVERSITE DE STRASBOURG - Strasbourg
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS - Urbana IL

International Classification:

C12N 5/071

US Classification:

435349, 435375, 435366, 435354, 435353

Abstract:

The present invention relates to a method for tightly temporally controlling the biological activity of a protein of interest in a vertebrate, upon induction of the activity of a fusion protein comprising said protein of interest and an ERM polypeptide containing a mutated ligand binding domain of the human oestrogen receptor α, with a synthetic ligand that does not interfere with oestrogen signalling. In particular, the present invention concerns a method for generating tightly temporally-controlled targeted somatic mutations in a vertebrate, preferably a mouse, by inducing the activity of a fusion protein comprising a site-specific recombinase protein and an ERM polypeptide, with a synthetic ligand devoid of oestrogenic and anti-oestrogenic activities.

US Patent:

20120256102, Oct 11, 2012

Filed:

Mar 8, 2012

Appl. No.:

13/385828

Inventors:

Younghoon Kim - Champaign IL, US
Sung hoon Kim - Champaign IL, US
Melikhan Tanyeri - Champaign IL, US
John A. Katzenellenbogen - Urbana IL, US

Assignee:

The Board of Trustees of the University of Illinois - Urbana IL

International Classification:

C08G 69/48
G01N 33/566
G01N 21/64
G01N 33/53

US Classification:

2504591, 525451, 435 72, 436501, 435 71

Abstract:

The invention provides dendrimers, conjugates thereof, and methods of using dendrimer conjugates. In one embodiment, the invention provides novel polymeric dendrimers as a new class of fluorescent labels. The labels can include multiple fluorescent dye molecules conjugated to a single polymeric backbone or core, such as a dendrimer. The dendrimers can have regular or irregular branched polymeric network structures that allow for the chemical attachment of multiple dye molecules, multiple color dyes, and/or multiple functional groups, in a combinatorial fashion. The fluorescent dendritic nanoprobes (FDNs) thus provide a new class of fluorescent reporters for fluorescence microscopy and imaging.

US Patent:

48514020, Jul 25, 1989

Filed:

Feb 27, 1987

Appl. No.:

7/019935

Inventors:

Martin J. Jacobs - Terre Haute IN
John Katzenellenbogen - Urbana IL

Assignee:

International Minerals & Chemical Corp. - Northbrook IL

International Classification:

C07J 100
A61K 31565

US Classification:

514182

Abstract:

Estriol is administered to ruminants in dosages from about 0. 01-4. 0 mg/ruminant/day to promote growth and increase feed utilization efficiency.

US Patent:

40641503, Dec 20, 1977

Filed:

May 26, 1976

Appl. No.:

5/690090

Inventors:

John A. Katzenellenbogen - Urbana IL

Assignee:

University of Illinois Foundation - Urbana IL

International Classification:

C11C 100
C07C 5300

US Classification:

260413

Abstract:

Aliphatic acids containing an isoprenoid 1,5-diene moiety are prepared in high yields by the selective gamma alkylation of. alpha. ,. beta. -unsaturated acids with allylic electrophiles. The gamma-regioselectivity of the alkylation is controlled by the use of the dicopper(I) dienolates prepared from the. alpha. ,. beta. -unsaturated acids. The method offers a particularly facile means for synthesizing isoprenoid 1,5-diene natural products such as farnesoic acid by alkylation of senecioic acid with geranyl bromide; geranoic acid by alkylation of senecioic acid with 3,3-dimethallyl bromide; and dl-lanceol by alkylation of tiglic acid with an allylic bromide derived from dl-limonene. Such products find use in the synthesis of insect pheremones, insect juvenile hormones, and components of perfumes.

US Patent:

20210130320, May 6, 2021

Filed:

Jun 11, 2019

Appl. No.:

17/251771

Inventors:

Abhishek SHARMA - Edison NJ, US
Sarat CHANDARLAPATY - New York NY, US
Lucia WANG - Jersey City NJ, US
Shengjia LIN - Secaucus NJ, US
Weiyi TOY - New York NY, US
John KATZENELLENBOGEN - Urbana IL, US

Assignee:

STEVENS INSTITUTE OF TECHNOLOGY - Hoboken NJ
MEMORIAL SLOAN-KETTERING CANCER CENTER - New York NY
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS - Urbana IL

International Classification:

C07D 401/04
C07D 209/12
C07C 233/20
C07C 233/21
C07D 333/64
C07D 409/14

Abstract:

A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized.

US Patent:

20190002380, Jan 3, 2019

Filed:

Jan 6, 2017

Appl. No.:

16/067676

Inventors:

John A. Katzenellenbogen - Urbana IL, US
Benita Katzenellenbogen - Urbana IL, US
Sung Hoon Kim - Champaign IL, US
Philip Shaul - Richardson TX, US

International Classification:

C07C 39/17
C07C 39/06
C07C 235/34
C07C 39/42
C07C 255/47
A61P 35/00
A61P 25/00

Abstract:

Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.