Global Patent Index - EP 1021407 A1

EP 1021407 A1 2000-07-26 - SYNTHESIS OF CLASTO-LACTACYSTIN BETA-LACTONE AND ANALOGS THEREOF

Title (en)

SYNTHESIS OF CLASTO-LACTACYSTIN BETA-LACTONE AND ANALOGS THEREOF

Title (de)

HERSTELLUNG VON CLASTO-LACTACYSTIN-BETA-LACTON UND ANALOGA DAVON

Title (fr)

SYNTHESE DE CLASTO-LACTACYSTINE BETA-LACTONE ET DE SES ANALOGUES

Publication

EP 1021407 A1 (EN)

Application

EP 98940885 A

Priority

  • US 9816858 W
  • US 5584897 P
  • US 91211197 A
  • US 6735297 P

Abstract (en)

[origin: WO9909006A1] The present invention is directed to an improved synthesis of clasto-lactacystin- beta -lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin- beta -lactones, and analogs thereof and their use as proteosome inhibitors.

IPC 1-7 (main, further and additional classification)

C07D 207/46; C07D 263/14

IPC 8 full level (invention and additional information)

C07D 207/46 (2006.01); C07D 491/044 (2006.01); A61K 31/40 (2006.01); A61K 31/4015 (2006.01); A61K 31/407 (2006.01); A61K 31/421 (2006.01); A61P 9/10 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 35/04 (2006.01); A61P 43/00 (2006.01); C07B 61/00 (2006.01); C07C 69/675 (2006.01); C07C 231/10 (2006.01); C07C 231/14 (2006.01); C07C 233/82 (2006.01); C07C 235/80 (2006.01); C07C 237/06 (2006.01); C07C 247/04 (2006.01); C07D 207/28 (2006.01); C07D 263/14 (2006.01); C07D 263/16 (2006.01); C07D 491/04 (2006.01); C07C 233/83 (2006.01)

CPC (invention and additional information)

C07D 263/16 (2013.01); C07C 69/675 (2013.01); C07C 231/14 (2013.01); C07C 235/80 (2013.01); C07C 237/06 (2013.01); C07C 247/04 (2013.01); C07D 207/28 (2013.01); C07D 491/04 (2013.01); C07B 2200/07 (2013.01)

Combination set (CPC)

C07C 231/14 + C07C 233/83

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

EPO simple patent family

WO 9909006 A1 19990225; AU 749857 B2 20020704; AU 8906298 A 19990308; BR 9811304 A 20011113; CA 2301054 A1 19990225; CN 1271342 A 20001025; EP 1021407 A1 20000726; EP 1021407 A4 20010704; HU 0002724 A2 20010228; HU 0002724 A3 20010428; IL 134538 A 20051120; IL 134538 D0 20010430; JP 2001515064 A 20010918; NZ 503169 A 20011221

INPADOC legal status


2007-10-17 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20070301

2007-03-23 [REG HK WD] APPLICATIONS WITHDRAWN, DEEMED TO BE WITHDRAWN, OR REFUSED AFTER PUBLICATION IN HONG KONG

- Document: HK 1029587

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07D 207/46 20060101AFI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07D 263/14 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07D 491/04 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07D 207/28 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07D 263/16 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07C 235/80 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07C 237/06 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07C 247/04 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07C 69/675 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: C07C 231/14 20060101ALI20060929BHEP

2006-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: A61K 31/40 20060101ALI20060929BHEP

2003-01-15 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20021128

2001-07-04 [A4] SUPPLEMENTARY SEARCH REPORT

- Effective date: 20010518

2001-07-04 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A4

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

2001-07-04 [RIC1] CLASSIFICATION (CORRECTION)

- Free text: 7C 07D 207/46 A, 7C 07D 263/14 B, 7C 07D 491/04 B, 7C 07D 207/28 B, 7C 07D 263/16 B, 7C 07C 235/80 B, 7C 07C 237/06 B, 7C 07C 247/04 B, 7C 07C 69/675 B, 7C 07C 231/14 B, 7A 61K 31/40 B, 7C 07D 491/04 J, 7C 07D 305:00 J, 7C 07D 209:00 J

2000-07-26 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000314

2000-07-26 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE