Quinoline sulfide derivatives

Details Quinoline sulfide derivatives Quinoline sulfide derivatives

1999-02-01

2000-05-02

Seaman, D. Margaret

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

514312, A61K 3147, C07D21516

Patent

active

06057447&

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to novel quinoline sulfide derivatives represented by the formula I and having antibacterial activity against Helicobacter pylori or pharmaceutically acceptable salts thereof and antibacterial agents comprising quinoline sulfide derivatives as effective components: ##STR2## wherein R.sub.1 represents hydrogen or halogen atom, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or di C.sub.1 -C.sub.6 alkylamino; R.sub.2 and R.sub.3 respectively represent hydrogen atom or C.sub.1 -C.sub.6 alkyl; one of R.sub.4 and R.sub.5 represents hydroxyl group and the other represents hydrogen atom or CR.sub.4 R.sub.5 represents carbonyl; m and n are integers, m being 1 or 2, n being 0 or 1; Ar represents, in a case where n is 0, a group of the formula II or III ##STR3## wherein R.sub.6 represents hydrogen atom, C.sub.1 -C.sub.6 alkyl or di C.sub.1 -C.sub.6 alkylamino; R.sub.7 represents hydrogen atom, C.sub.1 -C.sub.9 alkyl, hydroxy C.sub.1 -C.sub.6 alkyl, napthoyl C.sub.1 -C.sub.6 alkyl, acetoxy C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, trihalo C.sub.1 -C.sub.6 alkoxycarbonyl, di C.sub.1 -C.sub.6 alkylaminoacetyl or di C.sub.1 -C.sub.6 alkylamino C.sub.1 -C.sub.6 alkyl; R.sub.8 represents hydrogen atom, C.sub.1 -C.sub.6 alkyl, hydroxy C.sub.1 -C.sub.6 alkyl or acetoxy C.sub.1 -C.sub.6 alkyl, or NR.sub.7 R.sub.8 represents pyrrolidinyl, piperidino, morpholino or piperazinyl (which may be substituted by C.sub.1 -C.sub.6 alkyl or formyl); R.sub.9 represents benzyl; and t is an integer and is 0 or 1; the formula IV, V or VI ##STR4## wherein R.sub.10 represents hydrogen atom, C.sub.1 -C.sub.6 alkyl, hydroxyl group, C.sub.1 -C.sub.6 alkoxy, epoxy C.sub.1 -C.sub.6 alkoxy, mono- or dihydroxy C.sub.1 -C.sub.6 alkoxy, phenyl, piperidinyl (which may be substituted by C.sub.1 -C.sub.6 alkylcarbonyl or C.sub.1 -C.sub.6 alkoxycarbonyl), or tetrahydropyridyl (which may be substituted by C.sub.1 -C.sub.6 alkylcarbonyl); R.sub.11 represents hydrogen atom, C.sub.1 -C.sub.6 alkoxy or benzyloxy; R.sub.12 represents hydrogen atom or C.sub.1 -C.sub.6 alkoxy; R.sub.13 represents hydrogen atom or C.sub.1 -C.sub.6 alkoxy; R.sub.14 represents C.sub.1 -C.sub.6 alkoxycarbonyl, phenyl (which may be substituted by C.sub.1 -C.sub.6 alkoxy), or benzoyl (which may be substituted by C.sub.1 -C.sub.6 alkyl); R.sub.15 represents hydrogen or halogen atom; R.sub.16 represents hydrogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylcarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl or pyrrolidinyl (which may be substituted by C.sub.1 -C.sub.6 alkoxycarbonyl); R.sub.17 represents hydrogen atom, C.sub.1 -C.sub.9 alkyl or benzyl, or NR.sub.16 R.sub.17 represents piperidino, morpholino, piperazinyl (which may be substituted by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylcarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, trihalo C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 alkenyloxycarbonyl, phenoxycarbonyl, benzyloxycarbonyl, amino C.sub.1 -C.sub.6 alkylcarbonyl (amino group may be substituted by C.sub.1 -C.sub.6 alkoxycarbonyl), cinnamoyl (which may be substituted by C.sub.1 -C.sub.6 alkoxy), C.sub.1 -C.sub.6 alkylcarbamoyl, di C.sub.1 -C.sub.6 alkylsulfamoyl, C.sub.1 -C.sub.6 alkylsulfonyl, di C.sub.1 -C.sub.6 alkylaminothiocarbonyl, pyrimidyl or phenyl (which may be substituted by halogen atom)), imidazolidinyl (which may be substituted by oxo or C.sub.1 -C.sub.6 alkyl) or homopiperazinyl (which may be substituted by C.sub.1 -C.sub.6 alkoxycarbonyl); p is an integer within a range of 0-5 and r is an integer within a range of 0-2; there is no case where all of R.sub.1, R.sub.2, R.sub.3, R.sub.10, R.sub.11 and R.sub.12 are hydrogen atoms when m and n are respectively 1, CR.sub.4 R.sub.5 is carbonyl and Ar is the group of the formula IV; R.sub.1 is not hydrogen or halogen atom nor C.sub.1 -C.sub.6 alkoxy when m is 1, n is 0 and Ar is 4-aminophenyl.


BACKGROUND ART

Helicobacter pylori is a spiral, short rod-shaped, gram-negative bacterium having monopolar and several sheathed flagella. The bacteria are

REFERENCES:
patent: 5773449 (1998-06-01), Konishi et al.
CA 121:57310, Pluta, 1994.
Chemical Abstracts 121:35356, Coghlan, 1994.
Chemical Abstracts 113:39736, Pluta, 1990.
Chemical Abstracts 112:55907, Coghlan, 989, 1989.
Chemical Abstracts 110:154170, Knoll, 1988.
Chemical Abstracts 62:16017g, Kwart.
Chemical Abstracts 52:11055d, Kwart.
Chemical Abstracts 51:17794b, Kulka.

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