2-AMINOINDANS AS SELECTIVE DOPAMINE D3 LIGANDS

WIPO Patent Application WO/1995/004713

A1

Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of formula (I), wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CF3, CN, SR5, SO2NH2, SO2NR5R6, SO2R5, -OCO-C1-C6 alkyl, -NCO-C1-C6 alkyl, -CH2O-C1-C6 alkyl, -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-C1-C6 alkyl, phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazol, halogen (Br, Cl, F, I), R6 or R1 and R2 together form -O(CH2)mO- (where m is 1-2) or -CH2(CH2)pCH2 - (where p is 1-4); (except that only one of R1 and R2 can be hydrogen, OCH3 or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p-thienyl (where p is 1-4), hydrogen (except that only one of R3 and R4 can be hydrogen in any such compound) or C1-C8 alkyl (except where R1 or R2 are hydrogen, OCH3 or OH); R5 is hydrogen, C1-C8 alkyl, C2-C4 alkenyl, C3-C8 cycloalkyl; and R6 is C1-C8 alkyl, C2-C4 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, or Aryl.

HAADSMA-SVENSSON SUSANNE R (US)
ANDERSSON BENGT R (SE)
SONESSON CLAS A (SE)
LIN CHIU-HONG (US)
WATERS R NICHOLAS (SE)
SVENSSON KJELL A I (US)
CARLSSON PER A E (SE)
HANSSON LARS OLOV (SE)
STJERNLOF NILS PETER (SE)

PCT/US1994/008046

February 16, 1995

July 21, 1994

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UPJOHN CO (US)
HAADSMA SVENSSON SUSANNE R (US)
ANDERSSON BENGT R (SE)
SONESSON CLAS A (SE)
LIN CHIU HONG (US)
WATERS R NICHOLAS (SE)
SVENSSON KJELL A I (US)
CARLSSON PER A E (SE)
HANSSON LARS OLOV (SE)
STJERNLOF NILS PETER (SE)

A61K31/135; A61K31/335; A61K31/357; A61K31/36; A61K31/40; A61K31/42; A61K31/421; A61P25/00; A61P25/18; A61P25/20; A61P25/28; A61P25/30; A61P43/00; C07C211/42; C07C215/42; C07C217/52; C07C217/74; C07C219/26; C07C223/04; C07D295/08; C07C225/20; C07C225/22; C07C229/50; C07C233/43; C07C233/44; C07C237/30; C07C237/48; C07C255/54; C07C255/58; C07C309/56; C07C309/65; C07C309/66; C07C309/73; C07C309/76; C07C311/08; C07C311/21; C07C311/37; C07C311/39; C07C317/32; C07C317/36; C07C323/30; C07C323/36; C07D207/325; C07D209/48; C07D263/32; C07D295/096; C07D295/12; C07D295/135; C07D317/58; C07D317/70; C07D319/14; C07D319/18; C07D333/20; C07D207/32; (IPC1-7): C07C211/42; C07C233/43; C07D207/32; A61K31/135; A61K31/165; A61K31/40; A61K31/435; C07C309/66; A61K31/18; C07C309/73; C07C229/50; C07C217/74; C07C237/48; C07C311/08; C07C311/21; C07D295/08; C07C225/20; C07C223/04

WO1990007490A1

1990-07-12

EP0538134A2	1993-04-21
US4192888A	1980-03-11
DE1545673A1	1969-08-28
EP0334538A1	1989-09-27
EP0402923A2	1990-12-19

J. E. SUNDEEN ET. AL.: "Selective Inhibition of the Monosynaptic Spinal Reflex by a Series of Hydroxylated Alkylaminoindans", JOURNAL OF MEDICINAL CHEMISTRY, vol. 20, no. 11, November 1977 (1977-11-01), WASHINGTON US, pages 1478 - 85
J. G. CANNON ET. AL.: "Assessment of a Potential Dopaminergic Prodrug Moiety in Several Ring Systems", JOURNAL OF MEDICINAL CHEMISTRY, vol. 29, no. 10, October 1986 (1986-10-01), WASHINGTON US, pages 2016 - 20
CHEMICAL ABSTRACTS, vol. 114, no. 19, 13 May 1991, Columbus, Ohio, US; abstract no. 177884q, S. MA ET. AL.: "Dopaminergic Structure-Activity Relationships of 2-Aminoindans and Cardiovascular Action and Dopaminergic Activity of 4-Hydroxy-5-methyl-2-di-N-propylaminoindan (RD-211)." page 17; column 1;
CHEMICAL ABSTRACTS, vol. 81, no. 19, 11 November 1974, Columbus, Ohio, US; abstract no. 120286s, P. A. CROOKS: "New Synthesis of 2-Aminoindans" page 503; column 1;
CHEMICAL ABSTRACTS, vol. 80, no. 21, 27 May 1974, Columbus, Ohio, US; abstract no. 120604y, U. EDLUNG: "Preparation of N-substituted 2-Aminoindans" page 406; column 2;

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