公开(公告)号：EP0432719A1

公开(公告)日：1991-06-19

申请号：EP90123796.6

申请日：1990-12-11

申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED

发明人： Hamer, Russell Richard Lee ,  Freed, Brian ,  Allen, Richard Charles

IPC分类号： C07C225/22 ,  C07C225/16 ,  C07C221/00 ,  C07C217/86 ,  A61K31/135

CPC分类号： C07C225/22 ,  C07C45/004 ,  C07C45/455 ,  C07C49/233 ,  C07C49/80 ,  C07C217/86 ,  C07C225/16

摘要： This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula

where Ar is aryl of the formula
where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF₃, NO₂ and u is an integer of 1 to 3; X and Y are independently CH₂-, -CF₂- or -CHF-; Z and W are independently -CH₂-, -O-, -CHOH-, or -CHF-; m, n, p, q and t are integers which are independently 0 or 1; R₁ is H or loweralkyl; R₂ and R₃ are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.

摘要翻译： 本发明涉及烷基氨基和式其中Ar是下式其中V是氢，卤素，低级烷基，低级烷氧基，CF 3的芳基的烷基氨基烷基二芳基，NO 2和u是1至3的整数; X和Y独立地是-CH 2 - 或-CF 2 -CHF-; Z和W独立地是-CH 2 - ，-O - ， - -CHOH-，或-CHF-; M，N，p，q和t均为整数哪个独立为0或1; R 1是H或低级烷基; R2和R3是低级烷基; 和其药学上可接受的酸加成盐和如果适用的几何和光学异构体和外消旋混合物。 如阿尔茨海默氏病：本发明显示可用作止痛剂和作为用于减轻各种存储器功能障碍，由降低的胆碱能功能，颜色为特征的药剂的化合物。

公开(公告)号：EP4247783A1

公开(公告)日：2023-09-27

申请号：EP21827263.1

申请日：2021-11-17

申请人： GILEAD SCIENCES, INC.

发明人： DIXON, Darryl D. ,  ISCHAY, Michael A. ,  JOHNSON, Trevor C. ,  MERIT, Jeffrey E. ,  REGENS, Christopher S. ,  STANDLEY, Eric A. ,  STEINHUEBEL, Dietrich P.

IPC分类号： C07C255/59 ,  C07C255/54 ,  C07C205/37 ,  C07C217/86 ,  C07D267/12 ,  C07D317/22

公开(公告)号：EP2285770A1

公开(公告)日：2011-02-23

申请号：EP09757755.5

申请日：2009-06-02

申请人： Cipla Limited

发明人： HALDAVANEKAR, Vaman, Vaishali ,  PRABHU, Mangesh ,  RAO, Dharmaraj, Ramachandra ,  KANKAN, Rajendra, Narayanrao

IPC分类号： C07C213/00 ,  C07C213/08 ,  C07C213/10 ,  C07C217/86 ,  C07C231/02 ,  C07C233/43 ,  A61K31/167 ,  A61P11/00

CPC分类号： C07C231/10 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/08 ,  C07C213/10 ,  C07C217/60 ,  C07C217/86 ,  C07C231/02 ,  C07C233/43

摘要： The present invention provides a process for preparing a compound of formula (Vl) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (Vl), wherein the reduction is carried out in the presence of either (1 ) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein: R1 and R2 are independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo.

公开(公告)号：EP1359181B1

公开(公告)日：2010-07-21

申请号：EP01272334.2

申请日：2001-12-26

申请人： Nissan Chemical Industries, Ltd.

发明人： HOSAKA, Kazuyoshi, c/o Nissan Chemical Indu. Ltd. ,  NAWATA, Hideyuki, c/o Nissan Chemical Indu. Ltd. ,  NIHIRA, Takayasu, c/o Nissan Chemical Indu. Ltd.

IPC分类号： C08G73/10 ,  G02F1/1337 ,  C07C217/86 ,  C07C229/60

CPC分类号： G02F1/133723 ,  C07C217/86 ,  C07C229/60 ,  C08G73/10 ,  Y10T428/10 ,  Y10T428/1005 ,  Y10T428/1023 ,  Y10T428/31721

公开(公告)号：EP1359890A4

公开(公告)日：2009-08-12

申请号：EP02720821

申请日：2002-01-18

申请人： P & G CLAIROL INC

发明人： LIM MU-ILL ,  PAN YUH-GUO

IPC分类号： A61K8/00 ,  A61K8/33 ,  A61K8/34 ,  A61K8/41 ,  A61K8/49 ,  A61Q5/10 ,  C07C213/02 ,  C07C217/76 ,  C07C217/86 ,  C07D213/65 ,  C07D307/58 ,  C07D319/08 ,  C07D319/18 ,  C07D333/32 ,  D06P3/08 ,  A61K7/13

CPC分类号： C07D319/08 ,  A61K8/347 ,  A61K8/411 ,  A61K8/415 ,  A61K8/49 ,  A61K8/4926 ,  A61K8/494 ,  A61K8/4973 ,  A61K8/4986 ,  A61Q5/10 ,  C07D213/65 ,  C07D307/58 ,  C07D319/18 ,  C07D333/32

摘要： Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is hydrogen, hydroxy, nitro, amino, halogen, C1 to C5 alkyl or haloalkyl, C1 to C5 alkoxy, C1 to C5 hydroxyalkyl and C1 to C5 hydroxyalkoxy; Ar is an aromatic group, preferably an aromatic group selected from a furanyl, thienyl, pyridinyl, phenyl, 2,3-dihydrobenzo[1,4]dioxin-5 or 6-yl or benzo[1,3]dioxol-4 or 5-yl group; and y =1 to 3.

公开(公告)号：EP1052238A4

公开(公告)日：2007-05-02

申请号：EP99900676

申请日：1999-01-26

申请人： SHIONOGI & CO

发明人： TANIMOTO NORIHIKO ,  HASEGAWA YASUSHI ,  HAGA NOBUHIRO

IPC分类号： C07C43/215 ,  A61K31/07 ,  A61K31/075 ,  A61P37/00 ,  C07C43/20 ,  C07C43/23 ,  C07C43/285 ,  C07C49/84 ,  C07C205/38 ,  C07C215/76 ,  C07C215/82 ,  C07C217/54 ,  C07C217/58 ,  C07C217/80 ,  C07C217/84 ,  C07C217/86 ,  C07C217/90 ,  C07C233/25 ,  C07D213/30 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D231/12 ,  C07D237/12 ,  C07D237/14 ,  C07D239/26 ,  C07D239/36 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D277/06 ,  C07D307/38 ,  C07D333/06 ,  C07D401/10 ,  A61K31/44 ,  C07C43/295

CPC分类号： C07D401/10 ,  C07C43/20 ,  C07C43/23 ,  C07C215/76 ,  C07C215/82 ,  C07C217/54 ,  C07C217/58 ,  C07C217/84 ,  C07C217/86 ,  C07C217/90 ,  C07C233/25 ,  C07D213/30 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D231/12 ,  C07D237/12 ,  C07D237/14 ,  C07D239/26 ,  C07D239/36 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D277/06 ,  C07D307/38 ,  C07D333/06

摘要： A compound represented by formula (1) wherein each of ring A, ring B and ring C is independently a substituted or unsubstituted aromatic ring or a substituted or unsubstituted five or six-membered heterocycle which may be condensed with a benzene ring, when ring A, ring B and/or ring C is a substituted or unsubstituted five-membered heterocycle W1, W2 and/or W3 represents a bonding, X is D- or -NR1- (where R¿1? is hydrogen, a lower alkyl or the like), Y is hydrogen, a lower alkyl, a lower alkenyl or the like, and, for V?1 and V2¿ one is a single bond and the other is a single bond, -O- or the like, and a medicine comprising the compound.

公开(公告)号：EP0978506B1

公开(公告)日：2003-01-08

申请号：EP98911036.6

申请日：1998-03-26

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： OTA, Tomomi, Taisho Pharmaceutical Co., Ltd ,  NAKANISHI, Misa, Taisho Pharmaceutical Co., Ltd ,  TAGUCHI, Minoru, Taisho Pharmaceutical Co., Ltd ,  TOMISAWA, Kazuyuki, Taisho Pharmaceutical Co., Ltd

IPC分类号： C07C217/86 ,  C07C225/22 ,  C07C233/43 ,  C07C235/06 ,  C07C255/46 ,  C07C255/59 ,  A61K31/135 ,  A61K31/165 ,  A61K31/275 ,  A61K31/245

CPC分类号： C07C225/22 ,  C07C217/90 ,  C07C233/43 ,  C07C235/34 ,  C07C255/59 ,  C07C2601/02

摘要： 2-Phenoxyaniline derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein R represents a hydrogen atom, an amino group, or an NHCOR group; and R represents a halogen atom, an amino group, a cyano group, a C1-6 alkyl group, a C1-3 perfluoroalkyl group, an NHCOR group, a CH2OR group, an OCH2R group, or a COR group (wherein R represents a C1-6 alkyl group; R represents a hydrogen atom or a C1-6 alkyl group; R represents a hydrogen atom, a C1-6 alkyl group, a C1-5 aminoalkyl group, a C2-7 alkoxycarbonyl group, or a carbamoyl group; and R represents a C1-6 alkyl group, or an unsubstituted or (halogen, amino, cyano, or C1-6 straight-chain or branched alkyl)-substituted C3-8 cycloalkyl group).

摘要翻译： 由通式（I）表示的2-苯氧基苯胺衍生物或其药学上可接受的盐，其中R 1表示氢原子，氨基或NHCOR 3基团; R 2表示卤素原子，氨基，氰基，C 1-6烷基，C 1-3全氟烷基，NHCOR 3基，CH 2 OR 4基，OCH 2 R 5 >基或COR 6基（其中R 3表示C 1-6烷基; R 4表示氢原子或C 1-6烷基; R 5表示氢原子， C 1-6烷基，C 1-5氨基烷基，C 2-7烷氧基羰基或氨基甲酰基; R 6表示C 1-6烷基，或未取代的或（卤素，氨基，氰基或 C 1-6直链或支链烷基） - 取代的C 3-8环烷基）。

公开(公告)号：EP0938467B1

公开(公告)日：2002-06-12

申请号：EP97946623.2

申请日：1997-11-07

申请人： SEPRACOR, INC.

发明人： GAO, Yun ,  HETT, Robert ,  FANG, Kevin, Q. ,  WALD, Stephen, A. ,  SENANAYAKE, Chris, H.

IPC分类号： C07C231/18 ,  C07C233/43 ,  C07C213/02 ,  C07C217/86 ,  C07C233/25 ,  C07C205/37

CPC分类号： C07C233/25 ,  A61K9/0073 ,  C07B2200/07 ,  C07C59/255 ,  C07C201/12 ,  C07C205/37 ,  C07C205/45 ,  C07C213/02 ,  C07C217/86 ,  C07C231/02 ,  C07C231/18 ,  C07C233/43 ,  C07D303/36

摘要： A method is disclosed for the preparation of optically pure isomes of formeterol, especially the (R,R)- and (S,S)-isomer, by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy- alpha -methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as is the novel L-tartrate salt of R,R-formoterol.

公开(公告)号：EP0978506A1

公开(公告)日：2000-02-09

申请号：EP98911036.6

申请日：1998-03-26

申请人： TAISHO PHARMACEUTICAL CO. LTD

发明人： OTA, Tomomi, Taisho Pharmaceutical Co., Ltd ,  NAKANISHI, Misa, Taisho Pharmaceutical Co., Ltd ,  TAGUCHI, Minoru, Taisho Pharmaceutical Co., Ltd ,  TOMISAWA, Kazuyuki, Taisho Pharmaceutical Co., Ltd

IPC分类号： C07C217/86 ,  C07C225/22 ,  C07C233/43 ,  C07C235/06 ,  C07C255/46 ,  C07C255/59 ,  A61K31/135 ,  A61K31/165 ,  A61K31/275 ,  A61K31/245

CPC分类号： C07C225/22 ,  C07C217/90 ,  C07C233/43 ,  C07C235/34 ,  C07C255/59 ,  C07C2601/02

摘要： A 2-phenoxyaniline derivative represented by the formula:
wherein R 1 is a hydrogen atom, an amino group or an NHCOR 3 group, R 2 is a halogen atom, an amino group, a cyano group, a C 1-6 alkyl group, a C 1-3 perfluoroalkyl group, an NHCOR 3 group, a CH 2 OR 4 group, an OCH 2 R 5 group or a COR 6 group, R 3 is a C 1-6 alkyl group, R 4 is a hydrogen atom or a C 1-6 alkyl group, R 5 is a hydrogen atom, a C 1-6 alkyl group, a C 1-5 aminoalkyl group, a C 2-7 alkoxycarbonyl group or a carbamoyl group, and R 6 is a C 1-6 alkyl group or a C 3-8 cycloalkyl group which is unsubstituted or substituted by a halogen atom, an amino group, a cyano group or a straight or branched C 1-6 alkyl group; or a pharmaceutically acceptable salt thereof.

摘要翻译： 由下式表示的2-苯氧基苯胺衍生物：其中R1是氢原子，氨基或NHCOR3基团，R2是卤素原子，氨基，氰基，C1-6烷基，C1-3 全氟烷基，NHCOR3基，CH2OR4基，OCH2R5基或COR6基，R3为C1-6烷基，R4为氢原子或C1-6烷基，R5为氢原子，C1- 6烷基，C1-5氨基烷基，C2-7烷氧基羰基或氨基甲酰基，R6为未取代或被卤素原子取代的C1-6烷基或C3-8环烷基，氨基 基团，氰基或直链或支链C 1-6烷基; 或其药学上可接受的盐。

公开(公告)号：EP0484881B1

公开(公告)日：1999-04-07

申请号：EP91118838.1

申请日：1991-11-05

申请人： E.R. SQUIBB & SONS, INC.

发明人： Koster, William H. ,  Sundeen, Joseph E. ,  Straub, Henner ,  Ermann, Peter Hans ,  Treuner, Uwe D.

IPC分类号： C07D417/14 ,  A61K31/495 ,  C07D241/44 ,  C07D491/04 ,  C07F9/6509 ,  C07C271/66 ,  C07C217/86

CPC分类号： C07D241/52 ,  C07C217/86 ,  C07C271/66 ,  C07D241/44 ,  C07D417/14 ,  C07D491/04 ,  C07F9/650994 ,  Y02P20/55