Title:
2,4,6-TRISUBSTITUTED PYRIDINES WITH ESTROGENIC ACTIVITY AND METHODS FOR THE SOLID PHASE SYNTHESIS THEREOF
Document Type and Number:
WIPO Patent Application WO1999032447
Kind Code:
A3
Abstract:
The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z is selected from the group: n is an integer of a 1 or 2; R<1> is straight chain alkyl of 1 to 6 carbon atoms, branched chain alkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl, or phenyl substituted with fluoro, chloro, bromo, straight chain alkyl of 1 to 6 carbon atoms, branched chain alkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl, alkoxy of 1 to 6 carbon atoms, or methylenedioxy; and R<2> is furanyl, pyridyl, thieny, naphthalenyl, phenyl, or phenyl substituted with fluoro, chloro, bromo, straight chain alkyl of 1 to 6 carbon atoms, branched chain alkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkoxy of 1 to 6 carbon atoms, or methylenedioxy, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Inventors:
CHIU CHINGFAN
TANG ZHILIAN
ELLINGBOE JOHN WATSON
TANG ZHILIAN
ELLINGBOE JOHN WATSON
Application Number:
PCT/US1998/026363
Publication Date:
October 14, 1999
Filing Date:
December 10, 1998
Export Citation:
Assignee:
AMERICAN HOME PROD (US)
International Classes:
C07D213/30; C07D213/36; C07D405/04; C07D409/14; (IPC1-7): C07D213/30; A61K31/44; C07D405/04; C07D409/14
Domestic Patent References:
| WO1996021656A1 | 1996-07-18 |
Foreign References:
| EP0792640A2 | 1997-09-03 |
Other References:
DATABASE WPI Section Ch Week 9503, Derwent World Patents Index; Class B03, AN 95-022440, XP002111168
OLEKHNOVICH E P ET AL: "Photoinitiated processes in 2-(2-hydroxyaryl)pyridine molecules. I. Synthesis, structure and physiochemical properties of 2-(2-hydroxyaryl)-4,6-diarylpyridines", RUSS. J. ORG. CHEM. (ENGL. TRANSL.), vol. 32, no. 7, 1996, pages 1055 - 1058, XP002111163
DILTHEY W ET AL: "Beitrag zur Kenntnis der o-Violone", J. PRAKT. CHEM., vol. 114, 1926, pages 153 - 178, XP002111164
DILTHEY W ET AL: "Über arylierte Pyridine und ihre Beziehungen zu den entsprechenden Pyryliumverbindungen. IV.", J. PRAKT. CHEM., vol. 104, 1922, pages 28 - 36, XP002111165
DILTHEY W ET AL: "Über arylierte Pyridine und ihre Beziehungen zu den entsprechenden Pyryliumverbindungen. II.", J. PRAKT CHEM., vol. 102, 1921, pages 209 - 240, XP002111166
KROEHNKE F: "Synthesis using pyridinium salts . 5. The specific synthesisof pyridines and oligopyridines.", SYNTHESIS, no. 1, 1976, pages 1 - 25, XP002111167
OLEKHNOVICH E P ET AL: "Photoinitiated processes in 2-(2-hydroxyaryl)pyridine molecules. I. Synthesis, structure and physiochemical properties of 2-(2-hydroxyaryl)-4,6-diarylpyridines", RUSS. J. ORG. CHEM. (ENGL. TRANSL.), vol. 32, no. 7, 1996, pages 1055 - 1058, XP002111163
DILTHEY W ET AL: "Beitrag zur Kenntnis der o-Violone", J. PRAKT. CHEM., vol. 114, 1926, pages 153 - 178, XP002111164
DILTHEY W ET AL: "Über arylierte Pyridine und ihre Beziehungen zu den entsprechenden Pyryliumverbindungen. IV.", J. PRAKT. CHEM., vol. 104, 1922, pages 28 - 36, XP002111165
DILTHEY W ET AL: "Über arylierte Pyridine und ihre Beziehungen zu den entsprechenden Pyryliumverbindungen. II.", J. PRAKT CHEM., vol. 102, 1921, pages 209 - 240, XP002111166
KROEHNKE F: "Synthesis using pyridinium salts . 5. The specific synthesisof pyridines and oligopyridines.", SYNTHESIS, no. 1, 1976, pages 1 - 25, XP002111167
Download PDF: