CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC UREA AND AMIDE DERIVATIVES

Title:

CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC UREA AND AMIDE DERIVATIVES

Document Type and Number:

WIPO Patent Application WO2000066103

Kind Code:

Abstract:

This invention concerns cyclic combination therapies using indoline derivatives which are progesterone receptor antagonists of general structure (I) wherein: A, B and D are N or CH, though not all can be CH; R<1> and R<2> are H, COR, NRCOR, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R<1> and R<2> form a spirocyclic ring; R is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R is H, alkyl alkyl; R<3> is H, OH, NH2, alkyl, alkenyl, or COR; R is H, alkyl, aryl, alkoxy, or aminoalkyl; R<4> is benzene or a 5 or 6 memebered heteroaromatic ring; R is H, alkyl, aryl, alkoxy, or aminoalkyl; R is H or alkyl; R<5> is H or alkyl; W is O or a chemical bond; or a pharmaceutically acceptable salt thereof. These methods may be used for contraception or treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.

Inventors:

GRUBB GARY S (US)
ZHI LIN (US)
JONES TODD K (US)
TEGLEY CHRISTOPHER M (US)
PUWEN ZHANG (US)
FENSOME ANDREW (US)
VIET ANDREW Q (US)
SANTILLI ARTHUR A (US)
TEREFENKO EUGENE A (US)
WROBEL JAY E (US)
EDWARDS JAMES P (US)

Application Number:

PCT/US2000/011449

Publication Date:

April 05, 2001

Filing Date:

May 01, 2000

Export Citation:

Click for automatic bibliography generation

Assignee:

AMERICAN HOME PROD (US)
LIGAND PHARM INC (US)
GRUBB GARY S (US)
ZHI LIN (US)
JONES TODD K (US)
TEGLEY CHRISTOPHER M (US)
PUWEN ZHANG (US)
FENSOME ANDREW (US)
VIET ANDREW Q (US)
SANTILLI ARTHUR A (US)
TEREFENKO EUGENE A (US)
WROBEL JAY E (US)
EDWARDS JAMES P (US)

International Classes:

C07D498/04; A61K31/5365; A61K31/565; A61K31/57; A61K45/06; A61P5/32; A61P5/36; A61P15/08; A61P15/18; A61P35/00; (IPC1-7): A61K45/06; A61K31/57; A61K31/565; A61P15/18; A61K31/495; A61K31/12

Domestic Patent References:

WO1996015794A1 1996-05-30
WO1997049407A1 1997-12-31

Foreign References:

DE4330234A1 1995-03-09
US5521166A 1996-05-28
US5733902A 1998-03-31
DE4344463A1 1995-06-29
US5696133A 1997-12-09

Other References:

JHALANI, VINOD K. ET AL: "A convenient synthesis of 5-keto-6-methyl-5,6-dihydro-1,6-naphthyridine", INDIAN J. CHEM., SECT. B (1983), 22B(9), 916, XP000965424

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DE4330234A1	1995-03-09
US5521166A	1996-05-28
US5733902A	1998-03-31
DE4344463A1	1995-06-29
US5696133A	1997-12-09