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Title:
ADENOSINE A3 RECEPTOR AGONISTS
Document Type and Number:
WIPO Patent Application WO/2003/014137
Kind Code:
A1
Abstract:
Disclosed are novel compounds of the Formula I that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia. Formula (I) wherein: R?1¿ is optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; X is a covalent bond or optionally substituted alkylene; R?1¿ is R?4¿ Z-Y-C=C- or optionally substituted pyrazolyl: in which Y is optionally substituted alkylene, Z is oxygen, sulfur or NH-, and R?4¿ is optionally substituted aryl or optionally substituted heteroaryl; and R?3¿ is hydroxymethyl or C(0)-NR?5¿R?6¿; in which R?5¿ and R?6¿ are independently hydrogen or lower alkyl.

Inventors:
ELZEIN ELFATIH
PALLE VENKATA
VARKHEDKAR VAIBHAV
ZABLOCKI JEFF
Application Number:
PCT/US2002/024696
Publication Date:
February 20, 2003
Filing Date:
August 06, 2002
Export Citation:
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Assignee:
CV THERAPEUTICS INC (US)
International Classes:
A61K31/7076; A61P7/00; A61P9/00; A61P13/12; C07H19/173; A61P15/08; A61P25/00; A61P35/00; A61P43/00; C07H19/16; (IPC1-7): C07H19/16; A61K31/70; A61P35/00
Domestic Patent References:
WO2000078777A12000-12-28
WO2000078778A22000-12-28
WO2000078779A22000-12-28
Other References:
KLOTZ K-N ET AL: "2-SUBSTITUTED N-ETHYLCARBOXAMIDOADENOSINE DERIVATIVES AS HIGH-AFFINITY AGONISTS AT HUMAN A3 ADENOSINE RECEPTORS", NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY, SPRINGER, BERLIN, DE, vol. 360, no. 2, 1999, pages 103 - 108, XP000984051, ISSN: 0028-1298
BARALDI P G ET AL: "NOVEL N6-(SUBSTITUTED-PHENYLCARBAMOYL)ADENOSINE-5'-URONAMIDES AS POTENT AGONIST FOR A3 ADENOSINE RECEPTORS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 39, no. 3, February 1996 (1996-02-01), pages 802 - 806, XP002913657, ISSN: 0022-2623
Attorney, Agent or Firm:
Clarke, Pauline (Inc. 3172 Porter Driv, Palo Alto CA, US)
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