Global patent index - EP 1015438 A4

EP 1015438 A4 2000-11-08 - PROTEASE INHIBITORS

Title (en)

PROTEASE INHIBITORS

Title (de)

PROTEASE INHIBITOREN

Title (fr)

INHIBITEURS DE PROTEASES

Publication

EP 1015438 A4 (EN)

Application

EP 98945850 A

Priority

  • US 9818289 W
  • US 5752797 P

Abstract (en)

[origin: WO9911637A1] The present invention provides compounds of Formula (I) wherein X, X1, X2, and X3 are independently selected from -H, -C1-6alkyl, -C1-6alkyl substituted by 1-3 fluorines, -C3-7cycloalkyl, -CN, -C(O)R1, -C(O)OR1, -C(O)NR1R2, -C(NR1)NR1R2, -C(NCN)NR1R2, -C(NCN)SR3, -NO2, -NR1SO2R3, -NR1C(O)R1, -NR1R2, -NR1(C=NR1)NR1R2, -NR1C(O)NR1R2, -NR1C(O)R1, -NR1C(O)OR3, -NR1C(NCN)SR3, -NR1C(NCN)NR1R2, -NR1C(O)C(O)NR1R2, -NR1C(O)C(O)R2, -Cl, -Br, -I, -F, -OR1, -O(CH2)qOR3, -O(CH2)2OH, -OC(O)R1, -O(CH2)qC(O)NR1R2, -O(CH2)qC(O)R1, -SR1, -SO2NR1R2 or -S(O)mR3; m is 0, 1 or 2; q is 1 or 2; n is 0 to 2; R1 is -H, -C1-6alkyl, -CF3 or -CH2CF3; or when R1 and R2 are taken together as NR1R2, they may together with the nitrogen form a 5 to 7 membered ring comprised of carbon or carbon and one or more additional heteroatoms selected from O, N, or S; R2 is H, -C1-6alkyl, -CF3 or -CH2CF3; R3 is -C1-6alkyl, -CF3 or -CH2CF3; and X4 is -H, -C1-6alkyl, -C3-7cycloalkyl, -COAr, -COOC1-6alkyl, or COOAr; which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease therewith.

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

C07D 277/48; A61K 31/425

IPC 8 full level (invention and additional information)

C07D 277/20 (2006.01); A61K 31/426 (2006.01); A61K 31/427 (2006.01); A61P 1/02 (2006.01); A61P 19/02 (2006.01); A61P 19/08 (2006.01); A61P 19/10 (2006.01); A61P 29/00 (2006.01); A61P 43/00 (2006.01); C07D 277/42 (2006.01); C07D 277/48 (2006.01)

CPC (invention and additional information)

C07D 277/48 (2013.01)

Citation (search report)

  • [A] PATENT ABSTRACTS OF JAPAN vol. 009, no. 091 (C - 277) 19 April 1985 (1985-04-19)
  • See also references of WO 9911637A1

Designated contracting state (EPC)

BE CH DE ES FR GB IT LI NL

EPO simple patent family

WO 9911637 A1 19990311; AU 9300298 A 19990322; CA 2302361 A1 19990311; CO 4970736 A1 20001107; EP 1015438 A1 20000705; EP 1015438 A4 20001108; JP 2001514257 A 20010911; MA 26540 A1 20041220; PE 115699 A1 20000113; ZA 9808064 B 19990528

INPADOC legal status

2007-04-20 [REG HK WD] APPLICATIONS WITHDRAWN, DEEMED TO BE WITHDRAWN, OR REFUSED AFTER PUBLICATION IN HONG KONG

- Ref Legal Event Code: WD

- Ref Document Number: 1030414

- Country of Ref Document: HK

2004-08-04 [18D] DEEMED TO BE WITHDRAWN

- Ref Legal Event Code: 18D

- Effective date: 20040129

2003-11-05 [17Q] FIRST EXAMINATION REPORT

- Ref Legal Event Code: 17Q

- Effective date: 20030918

2000-11-08 [A4] SUPPLEMENTARY SEARCH REPORT

- Ref Legal Event Code: A4

- Effective date: 20000927

2000-11-08 [AK] DESIGNATED CONTRACTING STATES:

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- Designated State(s): BE CH DE ES FR GB IT LI NL

2000-11-08 [RIC1] CLASSIFICATION (CORRECTION)

- Ref Legal Event Code: RIC1

- Free Format Text: 7C 07D 277/48 A, 7A 61K 31/425 B

2000-07-05 [17P] REQUEST FOR EXAMINATION FILED

- Ref Legal Event Code: 17P

- Effective date: 20000301

2000-07-05 [AK] DESIGNATED CONTRACTING STATES:

- Ref Legal Event Code: AK

- Designated State(s): BE CH DE ES FR GB IT LI NL