Global patent index - EP 1073632 A1

EP 1073632 A1 2001-02-07 - SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS

Title (en)

SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS

Title (de)

SUBSTITUIERTE BENZAMIDE,DEREN HERSTELLUNG UND ANWENDUNG ALS INHIBITOREN VON CYSTEIN-PROTEASEN

Title (fr)

BENZAMIDES SUBSTITUES, LEUR PRODUCTION ET LEUR UTILISATION COMME INHIBITEURS DE PROTEASES DE CYSTEINE

Publication

EP 1073632 A1 (DE)

Application

EP 99920704 A

Priority

  • DE 19817461 A
  • EP 9902617 W

Abstract (en)

[origin: DE19817461A1] Benzamide derivatives (I) are new. Benzamide derivatives of formula (I) and their tautomers, isomers and salts are new: R<1> = 1-6C alkyl optionally monosubstituted by Ar, cyclohexyl, indolyl or SMe; Ar = phenyl optionally substituted by 1-2 R<4> groups; R<4> = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CN, COOH, 2-5C alkoxycarbonyl or 2-5C alkanoylamino; R<2> = N(R<5>)COR<6> or N(R<5>)SO2R<6>; R<3> = halogen, 1-6C alkyl, 2-5C alkanoylamino, 1-4C alkylsulfonylamino, NO2, 1-4C alkoxy, CN, COOH, CONH2, 2-5C alkoxycarbonyl, 1-4C alkylsulfonyl, phenylsulfonyl, 1-4C alkylsulfamoyl, SO2NH2 or NH2; A = aryl or heteroaryl, e.g. naphthyl, quinolyl, quinoxalinyl, benzimidazolyl, benzothienyl, quinazolinyl, phenyl, thienyl, imidazolyl, pyridyl, pyrimidinyl or pyridazinyl, all optionally substituted by R<9> and 0-2 R<8> groups; B = a bond; (CH2)m, (CH2)mQ(CH2)o, CH=CH, ethynylene, COCH=CH or NHCOCH=CH; Q = O, S, SO, SO2, CO, NHCO, CONH, NHSO2 or SO2NH; or A-B = a group of formula (i)-(iv): R<5> = H or 1-4C alkyl; R<6> = H, phenyl, naphthyl, or 1-6C alkyl optionally substituted by Ar; R<8> = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CF3, NO2, NH2, CN, COOH, 2-5C alkoxycarbonyl, 2-5C alkanoylamino, phenyl, benzamido, 1-4C alkylsulfonylamino, phenylsulfonylamino, 1-4C alkylsulfonyl, pyridyl or phenylsulfonyl; R<9> = H or (CH2)pR<12>; R<12> = pyrrolidinyl, morpholinyl, piperidyl, homopiperazinyl, NR<10>R<13> or 4-R<10>-1-piperazinyl; R<10> = 1-6C alkyl optionally substituted by Ar'; Ar' = phenyl optionally substituted by 1-2 R<11> groups; R<11> = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CF3, NO2, NH2, CN, COOH, 2-5C alkoxycarbonyl, 2-5C alkanoylamino, 1-4C alkylsulfonylamino or 1-4C alkylsulfonyl; R<13> = H or 1-6C alkyl; n = 0-2; m, q (sic; o and p are not defined) = 0-4.

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

C07C 311/21; A61K 31/18; A61K 31/44; C07C 233/78; C07D 213/56; C07D 295/08

IPC 8 full level (invention and additional information)

C07D 295/08 (2006.01); A61K 31/18 (2006.01); A61K 31/27 (2006.01); A61K 31/4409 (2006.01); A61K 31/4418 (2006.01); A61P 9/00 (2006.01); A61P 13/12 (2006.01); A61P 25/00 (2006.01); A61P 25/08 (2006.01); A61P 25/14 (2006.01); A61P 25/28 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 35/04 (2006.01); A61P 37/02 (2006.01); A61P 43/00 (2006.01); C07C 233/78 (2006.01); C07C 235/42 (2006.01); C07C 237/34 (2006.01); C07C 311/21 (2006.01); C07D 213/56 (2006.01); C07D 295/096 (2006.01)

CPC (invention and additional information)

C07D 295/096 (2013.01); C07C 233/78 (2013.01); C07C 235/42 (2013.01); C07C 237/34 (2013.01); C07C 311/21 (2013.01); C07D 213/56 (2013.01)

Citation (search report)

See references of WO 9954293A1

Designated contracting state (EPC)

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

EPO simple patent family

DE 19817461 A1 19991021; AU 3818699 A 19991108; AU 743245 B2 20020124; BG 104856 A 20010531; BR 9909776 A 20001219; CA 2328430 A1 19991028; CN 1306509 A 20010801; CZ 20003890 A3 20011114; EP 1073632 A1 20010207; HR P20000777 A2 20010630; HU 0101616 A2 20010928; HU 0101616 A3 20021028; ID 26305 A 20001214; IL 138676 D0 20011031; JP 2002512220 A 20020423; NO 20005265 A 20001019; NO 20005265 D0 20001019; PL 343466 A1 20010813; SK 14122000 A3 20010510; TR 200003069 T2 20090121; US 6436925 B1 20020820; WO 9954293 A1 19991028; ZA 200006758 B 20011212

INPADOC legal status

2004-10-20 [18D] DEEMED TO BE WITHDRAWN

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- Effective date: 20040414

2003-05-07 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: ABBOTT GMBH & CO. KG

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2002-11-06 [17Q] FIRST EXAMINATION REPORT

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- Effective date: 20020919

2001-02-07 [17P] REQUEST FOR EXAMINATION FILED

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- Effective date: 20000923

2001-02-07 [AK] DESIGNATED CONTRACTING STATES:

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

2001-02-07 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

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