公开(公告)号：EP0342665A3

公开(公告)日：1990-08-16

申请号：EP89108926.0

申请日：1989-05-18

Applicant: Takeda Chemical Industries, Ltd.

Inventor： Kanamaru, Tsuneo ,  Hida, Tsuneaki ,  Muroi,, Masayuki

IPC: C07C65/42 ,  A61K31/19 ,  A61K31/235 ,  C07D265/30

CPC classification number: C07D295/192 ,  C07C65/40 ,  C07C65/42 ,  C07C235/84 ,  C07D313/12

Abstract: A novel compound of the formula (I):
wherein R₁ is optionally esterified or amidated carboxyl; R₂, R₃ and R₄ are the same or different and are hydrogen or alkyl; A is fcrmyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R₁ is carboxyl, R₂, R₃ and R₄ are hydrogen and X is formyl are also disclosed.

公开(公告)号：EP0342665A2

公开(公告)日：1989-11-23

申请号：EP89108926.0

申请日：1989-05-18

Applicant: Takeda Chemical Industries, Ltd.

Inventor： Kanamaru, Tsuneo ,  Hida, Tsuneaki ,  Muroi,, Masayuki

IPC: C07C65/42 ,  A61K31/19 ,  A61K31/235 ,  C07D265/30

CPC classification number: C07D295/192 ,  C07C65/40 ,  C07C65/42 ,  C07C235/84 ,  C07D313/12

Abstract: A novel compound of the formula (I):
wherein R₁ is optionally esterified or amidated carboxyl; R₂, R₃ and R₄ are the same or different and are hydrogen or alkyl; A is fcrmyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R₁ is carboxyl, R₂, R₃ and R₄ are hydrogen and X is formyl are also disclosed.

Abstract translation: 式（I）的新型化合物：其中R 1任选被酯化或酰胺化的羧基; R2，R3和R4相同或不同，为氢或烷基; A是fcrmyl，羟基亚氨基甲基或羧基; 并且X是氢或卤素或其盐，其可用作芳香酶抑制剂或其生产的中间体。 制备式（I）化合物的方法和含有作为活性成分的式（I）化合物的芳香酶抑制剂的方法，其中A是甲酰基，X是氢，或其盐，以及能产生青霉素的青霉菌（Penicillium funiculosum） 还公开了其中R 1是羧基，R 2，R 3和R 4是氢并且X是甲酰基的化合物（I）。

公开(公告)号：EP0652868A1

公开(公告)日：1995-05-17

申请号：EP93917937.0

申请日：1993-07-28

Applicant: RHONE-POULENC RORER LIMITED

Inventor： FENTON, Garry ,  MORLEY, Andrew David ,  PALFREYMAN, Malcolm Norman ,  RATCLIFFE, Andrew James ,  SHARP, Brian William ,  STUTTLE, Keith Alfred, James ,  THURAIRATNAM, Sukanthini ,  VACHER, Bernard Yvon Jack

IPC: C07D239 ,  A61K31 ,  A61P1 ,  A61P7 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P29 ,  A61P43 ,  C07C43 ,  C07C45 ,  C07C47 ,  C07C49 ,  C07C59 ,  C07C65 ,  C07C69 ,  C07C205 ,  C07C217 ,  C07C233 ,  C07C235 ,  C07C245 ,  C07C255 ,  C07C275 ,  C07C311 ,  C07C317 ,  C07C321 ,  C07C323 ,  C07C327 ,  C07D213 ,  C07D241 ,  C07D261 ,  C07D275 ,  C07D409

CPC classification number: C07D213/75 ,  C07C43/225 ,  C07C45/004 ,  C07C45/292 ,  C07C45/71 ,  C07C47/575 ,  C07C49/84 ,  C07C59/58 ,  C07C59/60 ,  C07C59/62 ,  C07C65/21 ,  C07C65/24 ,  C07C65/42 ,  C07C69/76 ,  C07C69/92 ,  C07C205/59 ,  C07C217/88 ,  C07C235/56 ,  C07C255/60 ,  C07C275/34 ,  C07C311/29 ,  C07C311/46 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07D213/50 ,  C07D213/89 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D275/03 ,  C07D409/12

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

公开(公告)号：EP0652868B1

公开(公告)日：2004-11-10

申请号：EP93917937.0

申请日：1993-07-28

Applicant: Aventis Pharma Limited

Inventor： FENTON, Garry ,  MORLEY, Andrew David ,  PALFREYMAN, Malcolm Norman ,  RATCLIFFE, Andrew James ,  SHARP, Brian William ,  STUTTLE, Keith Alfred, James ,  THURAIRATNAM, Sukanthini ,  VACHER, Bernard Yvon Jack

IPC: C07D213/75 ,  C07D213/89 ,  C07D213/50 ,  C07C49/84 ,  C07C233/67 ,  C07C275/34 ,  C07C69/92 ,  C07C43/243 ,  A61P29/00

CPC classification number: C07D213/75 ,  C07C43/225 ,  C07C45/004 ,  C07C45/292 ,  C07C45/71 ,  C07C47/575 ,  C07C49/84 ,  C07C59/58 ,  C07C59/60 ,  C07C59/62 ,  C07C65/21 ,  C07C65/24 ,  C07C65/42 ,  C07C69/76 ,  C07C69/92 ,  C07C205/59 ,  C07C217/88 ,  C07C235/56 ,  C07C255/60 ,  C07C275/34 ,  C07C311/29 ,  C07C311/46 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07D213/50 ,  C07D213/89 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D275/03 ,  C07D409/12