Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-08-12
1994-06-14
Springer, David B.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514 18, 514357, 514414, 514397, 514419, 514405, 530331, 546148, 546264, 5483121, 548453, 548495, A61K 3700, A61K 3145, A61K 31415, A61K 31405, C07D20920, C07D40312, C07D40112, C07K 500
Patent
active
053210328
DESCRIPTION:
BRIEF SUMMARY
FIELD OF ART
The present invention relates to a new peptide compound and the salt thereof, and more precisely, to a new peptide compound and the salt thereof which has a pharmaceutical activity such as tachykinin antagonism, especially substance P compound antagonism, neurochinin A antagonism, neurochinin B antagonism, and the like, and the process for the preparation of the above compound and tachykinin antagonism agent which contain the above compound as an active ingredient.
BACKGROUND OF ART
The object of the present invention is to provide a new and useful peptide compound and the salt thereof which has a pharmaceutical activity such as tachykinin antagonism, especially substance P compound antagonism, neurochinin A antagonism, neurochinin B antagonism, and the like.
The another object of the present invention is to provide a process for the preparation of the above peptide compound and the salt thereof.
The further object of the present invention is to provide a tachykinin antagonism agent which contains the above peptide compound or the salt thereof as an active ingredient.
The still further object of the present invention is to provide a use of the above peptide compound or the salt thereof as a tachykinin antagonism agent, especially substance P antagonism agent, neurochinin A antagonism agent, neurochinin B antagonism agent, and the like which is useful for therapeutics or prevention of tachykinin interstitial diseases of human or animals such as respiratry diseases (e.g., asthma, bronchitis, thiniris, cough, expectoration, etc.), ophthalmic diseases (e.g., conjunctivitis, vernal conjunctivitis, etc.), cutaneous diseases (e.g., contact dermatitis, atopic dermatitis, urticaria, other kind of eczematoid dermatitis, etc.), inflammatory diseases (e.g., rheumatoid arthritis, osteoarthritis, etc.), pain or aches ( e.g., migraine, headache, toothache, cancerous pain, backpain, etc.), and the like.
DISCLOSURE OF THE INVENTION
The object compound of the present invention may be illustrated as the following general formula (I).
BEST MODE OF THE INVENTION
The object compound (I) of the present invention may be prepared by the method as illustrated as the following reaction scheme. ##STR1##
All the compounds (Ia), (Ib), (It), (Id), (Ie) and (If) illustrated on the above reaction scheme are included in the object compound (I) of the present invention. Accordingly, in the following explanation, these compounds (Ia)-(If) may be generally described as the object compound (I). All the compounds (IIa), (IIb) and (IIc) are used as the starting compound, and some of them are new and may be prepared according to the preparative examples described below or commonly used method.
In the present specification, amino acid, peptide, protective group, condensing agent may be illustrated by showing the abbreviation thereof that are defined at IUPAC-IUB.
In the case that amino acid or its residue is shown by using the above mentioned abbreviation without any specific instruction, it means compounds of L-form and D-form, compound and residue of D-form are shown with an indication of D-.
The suitable salt of the object compound (I) is a conventionally used non-toxic salt that include acid addition salt such as organic acid salt (e.g., acetic acid salt, trifuluoroacetic acid salt, maleic acid salt, tartaric acid salt, methanesulfonic acid salt, benzenesulfonic acid salt, formic acid salt, toluenesulfonic acid salt, etc.), inorganic acid salt (e.g., hydrochloric acid salt, hydrobromic acid salt, hydriodic acid salt, sulfuric acid salt, nitric acid salt, phosphoric acid salt, etc.), salt with amino acid (e.g., arginine, aspargic acid, gulutamic acid, etc.); metal salt such as alkali metal salt (e.g., sodium salt, pottasium salt, etc.,), alkaline earth metal salt (e.g., calcium salt, magnesium salt, etc.); ammonium salt; salt with organic base (e.g., trimethylamine, triethylamine, pyridine, picoline, dicyclohexylamine, N,N'-dibenzylethylenediamine, etc.); and the like.
Several definition used in the afore or below descrip
Hagiwara Daijiro
Matsuo Masaaki
Miyake Hiroshi
Fujisawa Pharmaceutical Co. Ltd.
Springer David B.
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