2-phenylpiperazine derivatives
First Claim
1. A 2-phenylpiperazine derivative represented by the following formula (I) or a pharmaceutically acceptable salt, thereof, said 2-phenylpiperazine derivative being represented by the formula (I):
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wherein each of X1 and X3 is oxygen or two hydrogen atoms, X2 is O, NH, NCH3, or CH2, n is an integer of 0 or 1, R1 is hydrogen or lower alkyl and R2 is hydrogen, cyano, tetrazolyl, aminotriazolyl, mesyl, t-butoxycarbonyl, or lower alkyl, wherein when R2 is lower alkyl, the lower alkyl may be optionally substituted with a substituent selected from the following substituents (a) to (j) and/or oxo,(a) triazolonyl, (b) tetrazolyl, (c) dimethylaminomethyltriazolyl;
(d) phosphotriazolonyl, (e) pyridyl, (f) dimethylamino, (g) cyano, (h) pyrrolidino, (i) amino, (j) phenyl, R3 is hydrogen, halogen, lower alkyl or lower alkoxy, each of R4 and R5 is hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond.
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Accused Products
Abstract
A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof:
wherein each of X1 and X3 is oxygen or two hydrogen atoms, X2 O, NH, NCH3, or CH2, n is an integer of 0 or 1, R1 is hydrogen or lower alkyl and R2 is hydrogen, cyano, tetrazolyl, aminotriazolyl , mesyl, t-butoxycarbonyl, or a lower alkyl which may be optionally substituted, R3 is hydrogen, halogen, lower alkyl or lower alkoxy, each of R4 and R5 is hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond. The derivative may be used as a tachykinin antagonist in the treatment of diseases of the digestive system, nervous system and respiratory system, inflammation, allergy, carcinoid syndrome, chronic pain, headache, Crohn disease, depression and vomiting.
9 Citations
18 Claims
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1. A 2-phenylpiperazine derivative represented by the following formula (I) or a pharmaceutically acceptable salt, thereof, said 2-phenylpiperazine derivative being represented by the formula (I):
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wherein each of X1 and X3 is oxygen or two hydrogen atoms, X2 is O, NH, NCH3, or CH2, n is an integer of 0 or 1, R1 is hydrogen or lower alkyl and R2 is hydrogen, cyano, tetrazolyl, aminotriazolyl, mesyl, t-butoxycarbonyl, or lower alkyl, wherein when R2 is lower alkyl, the lower alkyl may be optionally substituted with a substituent selected from the following substituents (a) to (j) and/or oxo, (a) triazolonyl, (b) tetrazolyl, (c) dimethylaminomethyltriazolyl;
(d) phosphotriazolonyl, (e) pyridyl, (f) dimethylamino, (g) cyano, (h) pyrrolidino, (i) amino, (j) phenyl, R3 is hydrogen, halogen, lower alkyl or lower alkoxy, each of R4 and R5 is hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 16, 17, 18)
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15. (5S,6S)-6-(3,5-Bis(trifluoromethyl)benzyloxymethyl)-1-methyl-4-(5-oxo-4,5-dihydro-1H-(1,2,4)triazol-3-ylmethyl)-5-phenylpiperazin-2-one.
Specification