ネガティブホルモン活性および/または拮抗薬活性を有するレチノイド化合物の合成と使用

Japanese Patent JP4295357

B2

The invention provides a compound of the formula wherein X is S, O, NR' where R' is H or alkyl of 1 to 6 carbons, or X is ÄC(R1)2Ün where R1 is independently H or alkyl of 1 to 6 carbons, and n is an integer between 0 and 2; R2 is hydrogen, lower alkyl of 1 to 6 carbons, F, Cl, Br, I, CF3, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons; R3 is hydrogen, lower alkyl of 1 to 6 carbons or F; m is an integer having the value 0-3; o is an integer having the value 0-3; Y is a phenyl or naphthyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, imidazolyl and pyrrazolyl, said phenyl and heteroaryl groups being optionally substituted with one or two R2 groups; A is (CH2)q where q is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, -CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, -COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, and R14 is (R15)r-phenyl, (R15)r-naphthyl, or (R15)r-heteroaryl where the heteroaryl group has 1 to 3 heteroatoms selected from the group consisting of O, S and N, r is an integer having the values of 0-5, and R15 is independently H, F, Cl, Br, I, NO2, N(R8)2, N(R8)COR8, NR8CON(R8)2, OH, OCOR8, OR8, CN, an alkyl group having 1 to 10 carbons, fluoro substituted alkyl group having 1 to 10 carbons, an alkenyl group having 1 to 10 carbons and 1 to 3 double bonds, alkynyl group having 1 to 10 carbons and 1 to 3 triple bonds, or a trialkylsilyl or trialkylsilyloxy group where the alkyl groups independently have 1 to 6 carbons; R16 is H, lower alkyl of 1 to 6 carbons; R17 is H, lower alkyl of 1 to 6 carbons, OH or OCOR11, and p is zero or 1, with the proviso that when p is 1 then there is no R17 substituent group, and m is an integer between 0 and 2.

Klein, Elliott S
Alan Tee, Johnson
Andrew M, Standeven
Beard, Richard Elle
Gillette, Samuel Jay
Duon, Thien Thi
Nagpal, Sunil
Vrygonda, Vidia Sagar
Ten, Min
Chandra Ratna, Roshanta A

JP51125897A

July 15, 2009

August 23, 1996

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ALLERGAN,INCORPORATED

C07C63/66; A61K31/15; C07D317/26; A61K31/192; A61K31/215; A61K31/216; A61K31/341; A61K31/352; A61K31/357; A61K31/37; A61K31/381; A61K31/382; A61K31/426; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4418; A61K31/47; A61K38/09; A61P5/00; A61P39/02; C07C57/50; C07C63/33; C07C63/331; C07C63/49; C07C63/72; C07C63/74; C07C65/19; C07C65/28; C07C65/38; C07C69/48; C07C69/618; C07C69/76; C07C69/773; C07C69/90; C07C69/94; C07C233/81; C07C245/10; C07C327/48; C07C335/06; C07C403/20; C07D213/55; C07D215/12; C07D277/20; C07D277/30; C07D307/54; C07D311/58; C07D333/24; C07D335/06; C07F7/08; C07C; C07D

JP8283238A
JP1305079A

CA2138000A1

Aoyama Aoi
Yasuo Shibata

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