Global Patent Index - EP 1019382 A1

EP 1019382 A1 2000-07-19 - COMPOUNDS AND COMPOSITIONS FOR TREATING DISEASES ASSOCIATED WITH SERINE PROTEASE, PARTICULARLY TRYPTASE, ACTIVITY

Title (en)

COMPOUNDS AND COMPOSITIONS FOR TREATING DISEASES ASSOCIATED WITH SERINE PROTEASE, PARTICULARLY TRYPTASE, ACTIVITY

Title (de)

MILDE FLÜSSIGE REINIGUNGSZUSAMMENSETZUNGEN IN FORM EINER MIKROEMULSION

Title (fr)

COMPOSES ET COMPOSITIONS POUR TRAITEMENT DE MALADIES ASSOCIEES A UNE SERINE PROTEASE, EN PARTICULIER UNE ACTIVITE DE TRYPTASE

Publication

EP 1019382 A1 (EN)

Application

EP 97954520 A

Priority

  • US 9721849 W
  • US 83367497 A

Abstract (en)

[origin: WO9845275A1] Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. A preferred aspect of the invention are compounds of Formula (II) in which: the dashed lines independently represent optional bonds; each R<2> independently is (C1-6)alkyl, (C1-6)alkyloxy, halo or hydroxy; each R<3> independently is (C1-6)alkyl, (C1-6)alkyloxy, halo or hydroxy; X<3> is -C(O)- or -CR<7>R<8>-, X<8> is -CH(R<1>)n1- or -C(R<1>)n1=, wherein R<1> is amino(N1-4)azolidinyl, amino(N1-4)azolyl, (N1-4)azolidinyl, (N1-4)azolyl, -NHC(NH)NR<9>R<9>, -C(NR<9>)R<9>, -C(NH)NHR<10>, -C(NH)NR<10>R<10> or -(CR<11>R<11>)yNH2, or X<8> is -N= or -NH(R<1>)n1-, wherein R<1> is -C(NR<9>)R<9>, -C(NH)NHR<10> or -C(NH)NR<10>R<10>, wherein each R<9> independently is hydrogen or (C1-6)alkyl and each R<10> independently is (C1-6)alkyl; and X<9> is -CH(R<4>)- or -C(R<4>)=, wherein R<4> is -R<12>, -OR<12>, -N(R<13>)R<12>, -SR<12>, -S(O)R<12>, -S(O)2R<12>, -S(O)2OR<12>, -S(O)2N(R<13>)R<12>, -N(R<13>)S(O)2R<12>, -C(O)R<12>, -C(O)OR<12>, -C(O)N(R<13>)R<12>, -N(R<13>)C(O)R<12>, -OC(O)N(R<13>)R<12>, -N(R<13>)C(O)OR<12>, -(CH2)n4N(R<13>)C(O)N(R<13>)R<12>, -OP(O)(OR<13>)OR<12> or -C(O)N(R<14>)CH(COOH)R<12>, or X<9> is -N= or -N(R<4>)-, wherein R<4> is -C(O)R<12>, -C(O)OR<12>, -C(O)N(R<13>)R<12>, -OC(O)N(R<13>)R<12> or -C(O)N(R<14>)CH(COOH)R<12>, wherein R<12>, R<13> and R<14> are as defined in the Summary of the Invention; R<5> is hydrogen or (C1-4)alkyl, R<6> is hydrogen or (C1-4) alkyl, which alkyl optionally is substituted with one to two substituents independently selected from (C1-4)alkyloxy, hydroxy and sulfo, R<7> is hydrogen or methyl and R<8> is hydrogen, methyl or hydroxy. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

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

C07D 235/20; A61K 31/415; C07D 401/14; C07D 403/14; C07D 413/06; C07D 413/14; C07D 471/04; C07D 498/04

IPC 8 full level (invention and additional information)

A61K 31/4184 (2006.01); A61K 31/437 (2006.01); A61K 31/517 (2006.01); A61K 31/5355 (2006.01); A61P 11/02 (2006.01); A61P 11/06 (2006.01); A61P 29/00 (2006.01); A61P 31/12 (2006.01); A61P 37/08 (2006.01); A61P 43/00 (2006.01); C07D 235/02 (2006.01); C07D 235/14 (2006.01); C07D 235/20 (2006.01); C07D 401/14 (2006.01); C07D 403/14 (2006.01); C07D 413/06 (2006.01); C07D 413/14 (2006.01); C07D 471/04 (2006.01); C07D 498/04 (2006.01); C07D 521/00 (2006.01); C07F 7/08 (2006.01)

CPC (invention and additional information)

C07D 231/12 (2013.01); C07D 233/56 (2013.01); C07D 235/20 (2013.01); C07D 249/08 (2013.01); C07D 401/14 (2013.01); C07D 403/14 (2013.01); C07D 413/06 (2013.01); C07D 413/14 (2013.01); C07D 471/04 (2013.01); C07F 7/0812 (2013.01)

Citation (search report)

See references of WO 9845275A1

Designated contracting state (EPC)

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

EPO simple patent family

WO 9845275 A1 19981015; AU 5895098 A 19981030; AU 752064 B2 20020905; CA 2285454 A1 19981015; CN 1251579 A 20000426; EE 04055 B1 20030616; EE 9900477 A 20000615; EP 1019382 A1 20000719; HU 0001522 A2 20010528; HU 0001522 A3 20010828; JP 2001519806 A 20011023; KR 20010006119 A 20010126; LT 4704 B 20000925; LT 99131 A 20000425; LV 12495 A 20000620; LV 12495 B 20010120; NO 314183 B1 20030210; NO 994858 A 19991206; NO 994858 D0 19991006; NZ 500029 A 20010223; PL 336233 A1 20000619; SI 20115 A 20000630; SK 136799 A3 20000711

INPADOC legal status


2004-09-01 [18D] DEEMED TO BE WITHDRAWN

- Ref Legal Event Code: 18D

- Effective date: 20040301

2001-06-27 [17Q] FIRST EXAMINATION REPORT

- Ref Legal Event Code: 17Q

- Effective date: 20010515

2000-07-19 [17P] REQUEST FOR EXAMINATION FILED

- Ref Legal Event Code: 17P

- Effective date: 19991029

2000-07-19 [AK] DESIGNATED CONTRACTING STATES:

- Ref Legal Event Code: AK

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