Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-06-18
2000-07-11
Lambkin, Deborah C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142282, 5142358, 544 60, 544 62, 544121, A61K 3154, A61K 31535, C07D41700, C07D41300
Patent
active
060873574
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to new piperazine derivatives and a pharmaceutically acceptable salt thereof.
More particularly, it relates to new piperazine derivatives and a pharmaceutically acceptable salt thereof which have pharmacological activities such as Tachykinin antagonism, especially Substance p antagonism, Neurokinin A antagonism, Neurokinin B antagonism, and the like, to a process for preparation thereof, to a pharmaceutical composition comprising the same, and to a use of the same as a medicament.
Accordingly, one subject of the present invention is to provide new and useful piperazine derivatives and a pharmaceutically acceptable salt thereof which have pharmacological activities such as Tachykinin antagonism, especially Substance P antagonism, Neurokinin A antagonism, Neurokinin B antagonism, and the like.
Another object of the present invention is to provide a process for the preparation of said piperazine derivatives and a salt thereof.
A further object of the present invention is to provide a pharmaceutical composition comprising, as an active ingredient, said piperazine derivatives and a pharmaceutically acceptable salt thereof.
Still further object of the present invention is to provide a use of said piperazine derivatives or a pharmaceutically acceptable salt thereof as Tachykinin antagonist, especially Substance P antagonist, Neurokinin A antagonist or Neurokinin B antagonist, useful for treating or preventing Tachykinin-mediated diseases, for example, respiratory diseases such as asthma, bronchitis, rhinitis, cough, expectoration, and the like; ophthalmic diseases such as conjunctivitis, vernal conjunctivitis, and the like; cutaneous diseases such as contact dermatitis, atopic dermatitis, urticaria, and other eczematoid dermatitis, and the like; inflammatory diseases such as rheumatoid arthritis, osteoarthritis, and the like; pains or aches (e.g., migraine, headache, toothache, cancerous pain, back pain, etc.); and the like in human being or animals.
BACKGROUND ART
Some piperazine derivatives having pharmaceutical activities such as Tachykinin antagonism have been known as described in EP 0655442 A1.
DISCLOSURE OF INVENTION
The object compound of the present invention can be represented by the following general formula (I): ##STR2## wherein Y is bond or lower alkylene, pyridyl(lower)alkylamino(lower)alkenyl; N-(lower alkyl)-N-[pyridyl(lower)alkyl]amino(lower)alkyl; triazolylamino(lower)alkyl; lower alkoxy(lower)alkylamino(lower)alkyl; bis[(lower)alkoxy(lower)alkyl]amino(lower)alkyl; N-(lower alkyl)-N-[(lower)alkoxy(lower)alkyl]amino(lower) alkyl; hydroxy(lower)alkyl; lower alkylsulfonyloxy(lower)alkyl; phenyl(lower)alkyl which may have lower alkanoyl, amino, lower alkanoylamino, di(lower)alkylaminocarbonyl or nitro; lower alkoxyphenyl (lower)alkylcarbonyl; lower alkanoylbenzoyl; benzoyl(lower)alkyl which has lower alkyl, chlorine or di(lower)alkylamino; benzoyl(lower)alkyl which has halogen and lower alkyl; dihalobenzoyl(lower)alkyl; di(lower)alkylbenzoyl(lower)alkyl; 3-fluorobenzoyl(lower)alkyl; 3-(4-fluorobenzoyl)propyl; 4,4-ethylenedioxy-4-(4-fluorophenyl)butyl; piperazinylcarbonyl(lower)alkyl which has cyclopentyl or halophenyl; (2-pyridyl) (lower)alkyl; (3-pyridyl)propyl; (3-pyridyl) (lower)alkynyl; imidazolyl(lower)alkyl which may have lower alkyl; pyrazolyl(lower)alkyl which may have lower alkyl; thiomorpholinylcarbonyl(lower)alkyl; (3-azabicyclo[3.2.2]non-3-yl)carbonyl(lower)alkyl; or thienylcarbonyl(lower)alkyl, 1,2,3,6-tetrahydropyridyl(lower)alkyl, 1,2,3,6-tetrahydropyridyl(lower)alkynyl, 1,2,3,4-tetrahydroisoquinolyl(lower)alkyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl(lower)alkyl, saturated heterocyclic(lower)alkyl, saturated heterocyclic(lower)alkenyl, saturated heterocyclic(lower)alkynyl, saturated heterocyclicamino(lower)alkyl, saturated heterocyclicamino(lower)alkenyl or saturated heterocyclicamino(lower)alkynyl, each of which may have suitable substituent(s),
It is to be noted that the object compound (I) may include one or more stereoisomers du
REFERENCES:
patent: 3935214 (1976-01-01), Zellner
patent: 5164388 (1992-11-01), De et al.
patent: 5238938 (1993-08-01), Tone et al.
patent: 5344830 (1994-09-01), Mills et al.
patent: 5670505 (1997-09-01), Matsuo et al.
patent: 5672602 (1997-09-01), Burkholder et al.
patent: 5840726 (1998-11-01), Burkholder et al.
patent: 5883098 (1999-03-01), Matsuo et al.
Igari Norihiro
Konishi Nobukiyo
Manabe Takashi
Matsuda Hiroshi
Matsuo Masaaki
Fujisawa Pharmaceutical Co. Ltd.
Lambkin Deborah C.
LandOfFree
Piperazine derivatives as tachykinin antagonists does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Piperazine derivatives as tachykinin antagonists, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Piperazine derivatives as tachykinin antagonists will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-542626