IPC분류정보
국가/구분 |
United States(US) Patent
등록
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국제특허분류(IPC7판) |
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출원번호 |
US-0875162
(2001-06-07)
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발명자
/ 주소 |
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출원인 / 주소 |
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대리인 / 주소 |
Oyen Wiggs Green & Mutala
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인용정보 |
피인용 횟수 :
26 인용 특허 :
22 |
초록
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Apparatus for tracking net consumption of calories by a user has an input to allow a user to enter the number of calories in food consumed by the user. The apparatus also includes a heart rate monitor and a timer. The heart rate monitor and timer. A processor in the apparatus can calculate the numbe
Apparatus for tracking net consumption of calories by a user has an input to allow a user to enter the number of calories in food consumed by the user. The apparatus also includes a heart rate monitor and a timer. The heart rate monitor and timer. A processor in the apparatus can calculate the number of calories expended by the user in an exercise session from the duration of the exercise session, as measured by the timer, and the intensity of the exercise session as measured by the timer. The apparatus may be provided as a light weight wrist wearable instrument. The apparatus simplifies tracking the expenditure of calories in exercise and makes it possible to vary dietary constraints on calorie consumption in accordance with the amount of exercise in which the user has participated.
대표청구항
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Apparatus for tracking net consumption of calories by a user has an input to allow a user to enter the number of calories in food consumed by the user. The apparatus also includes a heart rate monitor and a timer. The heart rate monitor and timer. A processor in the apparatus can calculate the numbe
Apparatus for tracking net consumption of calories by a user has an input to allow a user to enter the number of calories in food consumed by the user. The apparatus also includes a heart rate monitor and a timer. The heart rate monitor and timer. A processor in the apparatus can calculate the number of calories expended by the user in an exercise session from the duration of the exercise session, as measured by the timer, and the intensity of the exercise session as measured by the timer. The apparatus may be provided as a light weight wrist wearable instrument. The apparatus simplifies tracking the expenditure of calories in exercise and makes it possible to vary dietary constraints on calorie consumption in accordance with the amount of exercise in which the user has participated. another and each means a lower alkyl group, a carbamoyl group which may be substituted by 1 or 2 lower alkyl groups, or a lower alkyl-C(=O)-- or lower alkyl-O--C(=O)-- group, wherein R2and R3bind to optional carbon atoms on the ring, R4: this may be the same or different from one another and each means a hydrogen atom, a lower alkyl group, a carbamoyl group which may be substituted by 1 or 2 lower alkyl groups or a lower alkyl-C(=O)-- or lower alkyl-O--C(=O)-group, wherein R2and R3bind to optional carbon atoms on the ring, R5: a lower alkyl; aryl-lower alkyl-O--; carboxyl; lower alkyl-O--C(=O)--; amido which may be substituted by 1 or 2 lower alkyl groups; an aryl, a monocyclic or bicyclic five or six-membered heterocycle containing from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur, or cycloalkyl group each of the aryl, heterocycle and cycloalkyl is unsubstituted or substituted with 1 to 3 substitutents each selected from the group consisting of a halogen atom, halogeno-lower alkyl, lower alkyl, lower alkyl-O--, lower alkyl-S--, lower alkyl --S(O)--, lower alkyl-S(O)2--, sulfamoyl which may be substituted by 1 or 2 lower alkyl groups, halogeno-lower alkyl-O--, cyano, nitro, oxo(=O), lower alkyl-C(=O)--, aryl-C(=O)--, amino which may be substituted by 1 or 2 of lower alkyl or lower alkyl-C(=O)-- or lower alkyl-O--C(=O)--, aryl-O--, amino-O--, carbamoyl which may be substituted by 1 or 2 lower alkyl, or carboxyl or lower alkyl-O--C(=O)--, a monocyclic or bicyclic five or six-membered heterocycle containing from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur, and OH group(s); or N(R13)R14-lower alkyl-O--; with the proviso that when m=1, R4and R5may together form a five- or six-membered heterocycle which may have other hetero atoms, R6: a halogeno-lower alkyl; aryl; or lower alkyl which may be substituted by N(R9)R10,OH or lower alkyl-O--, R7: a lower alkyl, aryl or N(R11)R12 R8,R9,R10,R11,R12,R13and R14: hydrogen, lower alkyl or aryl, with the proviso that R6and R8,R9and R10or R13and R14may together form a nitrogen-containing cycloalkyl which may have other hetero atoms and which is unsubstituted or substituted with 1 to 3 substituents each selected from the group consisting of a halogen atom, halogeno-lower alkyl, lower alkyl, lower alkyl-O--, lower alkyl-S--, lower alkyl-S(O)--, lower alkyl-S(O)2--, sulfamoyl which may be substituted by 1 or 2 lower alkyl groups, halogeno-lower alkyl-O--, cyano, nitro, oxo(=O), lower alkyl-C(=O)--, aryl-C(=O)--, amino which may be substituted by 1 or 2 of lower alkyl or lower alkyl-C(=O)-- or lower alkyl-O--C(=O)--, aryl-O--, amino-O--, carbamoyl which may be substituted by 1 or 2 lower alkyl, or carboxyl or lower alkyl-O--C(=O)--, a monocyclic or bicyclic five or six-membered heterocycle containing from 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and sulfur atom which is unsubstituted or substituted with 1 to 2 substitutents each selected from the group consisting of an oxo group, a lower alkyl group, alkyl group, and an OH group, k: 2, n:1, m: 0 or 1, p: 0, 1 or 2, A: an oxygen atom or NR8, X: --C(=O)-- group, Y: a bond, lower alkylene, --C(=O)-- or --S(O)2-- group, with the proviso that, when R5is a lower alkyl group, Y is a group other than lower alkylene, and Z1or Z2: CH. 2. The cyanophenyl compound or a salt thereof according to claim 1, wherein R is a cyano group. 3. The cyanophenyl compound or a salt thereof according to claim 2, wherein R1is a halogen atom, cyano, halogeno-lower alkyl, nitro or lower alkyl-O--; R2 and R3: at least one of them is a lower alkyl group; R4: a hydrogen atom or a lower alkyl group; R5: an aryl, a monocyclic or bicyclic five- or six-membered heterocycle containing from 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, or cycloalkyl group, each of the aryl, heterocycle and cycloalkyl is unsubstituted or substituted with 1 to 3 substituents each selected from the group consisting of a halogen atom, halogeno-lower alkyl, lower alkyl, lower alkyl-O--, lower alkyl-S--, lower alkyl-S(=O)--, lower alkyl-S(O)2--, sulfamoyl which may be substituted by 1 or 2 lower alkyl groups, halogeno-lower alkyl-O--, cyano, nitro, oxo(=O), lower alkyl-C(=O)--, aryl-C(=O)--, amino which may be substituted by 1 or 2 of lower alkyl or lower alkyl-C(=O)-- or lower alkyl-O--C(=O)--, aryl-O--, amino-O--, carbamoyl which may be substituted by 1 or 2 lower alkyl or carboxyl or lower alkyl-O--C(=O)--, a monocyclic or bicyclic five- or six-membered heterocycle containing from 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, and OH group; k is 2, n is 1; m is 1, X is C(=O)-- group; Y is a bond; and Z1or Z2both means CH. 4. The cyanophenyl derivative according to claim 3, wherein the substituent group of the aryl, heterocyclic or cycloalkyl group of R5which may have a substituent group is a radical selected from the group consisting of a halogen atom, halogeno-lower alkyl, lower alkyl, lower alkyl-O--, lower alkyl-S--, lower alkyl-S(O)--, lower alkyl-S(O)2--, cyclopropyl, 2-morpholin-4-yl-ethoxy, sulfamoyl which may be substituted by 1 or 2 lower alkyl groups, halogeno-lower alkyl-O--, cyano, nitro, oxo(=O), lower alkyl-C(=O)--, aryl-C(=O)--, amino which may be substituted by 1 or 2 of lower alkyl or lower alkyl-C(=O)-- or lower alkyl-O--C(=O)--, aryl-O--, amino-O--, carbamoyl which may be substituted by lower alkyl, carboxyl, lower alkyl-O--C(=O)--, heterocycle, cyclopropyl and OH group(s). 5. A compound, or a salt thereof, selected from (2R,5S)-4-(4-cyano-3-trifluoromethylphenyl)-N-(6-methoxy-3-pyridyl)-2,5-dimethylpiperazine-1-carboxamide; (2R,5S)-N-(2-amino-4-pyimidin-4-yl)-4-(4-cyano-3-trifluoromethylphenyl)-2,5-dimethylpiperazine-1-carboxamide; (2R,5S)-4-(4-cyano-3-trifluoromethylphenyl)-2,5-dimethyl-N-(6-trifluoromethyl-3-pyridyl)piperazine-1-carboxamide; (2R,5S)-4-(4-cyano-3-trifluoromethylphenyl)-N-(2-fluoro-4-pyridyl)-2,5-dimethylpiperazine-1-carboxamide; 4-(4-cyano-3-trifluoromethylphenyl)-N-[2-(2-cyclopropyl-6-methoxy-4-pyridyl)-2,5-dimethylpiperazine-1-carboxamide; 4-(4-cyano-3-trifluoromethylphenyl)-2,5-dimethyl-N-[2-(2-morpholin-4-yl-ethoxy)-4-pyridyl]piperazine-1-carboxamide; and (2R,5S)-N-(2-bromo-4-pyridyl)-4-(4-cyano-3-trifluoromethylphenyl)-2,5-dimethylpiperazine-1-carboxamide. 6. A pharmaceutical composition for inhibiting binding to the androgen receptor, which comprises as an active ingredient the cyanophenyl compound of claim 1 or a pharmaceutically acceptable salt thereof in an amount sufficient for expressing an anti-androgen activity, and a pharmaceutically acceptable carrier. 7. A method for inhibiting binding to an androgen receptor, comprising administering to an animal as an active ingredient the cyanophenyl derivative of claim 1 or a pharmaceutically acceptable salt thereof in an amount sufficient for expressing an anti-androgen activity, and a pharmaceutically acceptable carrier. resented by the general formula (1): wherein Het represents an optionally substituted heterocyclic group; A1and A2each independently represent --CH=, etc.; A3represents --CH2--, etc.; R1represents a 4-fluorophenyl group, etc.; R2represents an alkyl group; n represents 0, 1 or 2, provided that when A1and A2both are --CH=, A3represents --CH2-- or --SO2--, which is an indole derivative or a mono- or diazaindole derivative that has COX-2 inhibitory activity and is useful as a pharmaceutical, such as an anti-inflammatory agent, or addition salts thereof with a pharmaceutically acceptable acid or base, or hydrates thereof.
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