公开(公告)号：EP0680950A4

公开(公告)日：1996-02-28

申请号：EP95900905

申请日：1994-11-16

申请人： KYOWA HAKKO KOGYO KK

发明人： IKEDA SHUN-ICHI ,  KIMURA UICHIRO ,  ASHIZAWA TADASHI ,  GOMI KATSUSHIGE ,  SAITO HIROMITSU ,  KASAI MASAJI

IPC分类号： C07D209/12 ,  C07D209/30 ,  C07D401/06 ,  C07D405/06 ,  A61K31/40 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D209/12 ,  C07D209/30 ,  C07D405/06

摘要： A propenone derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein R1 represents hydrogen, lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylsulfonyl, aralkyl, (un)substituted aroyl, (un)substituted arylsulfonyl, (un)substituted heteroarylcarbonyl, (un)substituted heteroarylsulfonyl, diglycolyl or a group of formula (a), R2 represents hydrogen, lower alkyl, halogen, (un)substituted aryl or (un)substituted heteroaryl; R3 represents hydrogen, lower alkyl or (un)substituted aryl; and R?4, R5, R6 and R7¿ represent each independently hydrogen, lower alkyl, lower alkoxy, aralkyloxy, hydroxy, nitro, halogen, trifluoromethyl or -NR8R9, wherein R?8 and R9¿ represent each independently hydrogen, lower alkyl, lower alkanoyl, lower alkoxycarbonyl or (un)substituted aroyl.

公开(公告)号：EP0678508A1

公开(公告)日：1995-10-25

申请号：EP95201691.3

申请日：1992-08-29

申请人： MERCK & CO. INC.

发明人： Williams, Theresa M. ,  Ciccarone, Terrence M. ,  Saari, Walfred S. ,  Wai, John S. ,  Greenlee, William J. ,  Balani, Suresh K. ,  Goldman, Mark E., Signal Phamaceuticals ,  Theoharides, Anthony D.

IPC分类号： C07D209/42 ,  C07D209/30 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  C07D401/06 ,  C07D405/06 ,  C07D413/06 ,  A61K31/40 ,  A61K31/44 ,  A61K31/41

CPC分类号： C07D231/12 ,  C07D209/12 ,  C07D209/30 ,  C07D209/42 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06

摘要： Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 新型吲哚化合物抑制HIV逆转录酶，可用于预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物组合，抗感染药物 ，免疫调节剂，抗生素或疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。

公开(公告)号：EP0563916B1

公开(公告)日：1995-08-16

申请号：EP93105332.6

申请日：1993-03-31

申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED

发明人： Kosley, Raymond W., Jr. ,  Flanagan, Denise M. ,  Martin, Lawrence Leo ,  Nemoto, Peter Allen

IPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/12 ,  C07D209/48 ,  A61K31/40

CPC分类号： C07D209/08 ,  A61K31/40 ,  C07D209/12 ,  C07D209/30

公开(公告)号：EP0639567A1

公开(公告)日：1995-02-22

申请号：EP93911947.5

申请日：1993-04-28

申请人： OTSUKA PHARMACEUTICAL FACTORY, INC.

发明人： INAI, Masatoshi 20-1, Aza Kitawake Yagami ,  SHIBUTANI, Tadanao 96-1, Aza Mitsuhokaitaku ,  KANAYA, Jun 22-7, Aza Higashibiraki Nakamura ,  MORITAKE, Masako 38-1, Nakashowa-cho 1-chome ,  TANAKA, Akie 32, Aza Hon-cho Bezaiten Muya-cho

IPC分类号： C07D209/10 ,  C07D209/30 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D401/12 ,  C07D209/10

摘要： An indole derivative represented by general formula (1). It has a potent antiestrogenic effect and hence is useful for treating estrogen-dependent diseases such as anovular infertility, prostatomegaly, osteoporosis, breast cancer, endometrial cancer and melanoma.

摘要翻译： 由通式（1）表示的吲哚衍生物。 它具有有效的抗雌激素作用，因此可用于治疗雌激素依赖性疾病，如无性生殖不全，前列腺肥大，骨质疏松症，乳腺癌，子宫内膜癌和黑素瘤。

公开(公告)号：EP0576349A1

公开(公告)日：1993-12-29

申请号：EP93401602.3

申请日：1993-06-22

申请人： SANOFI

发明人： Gubin, Jean ,  Renard, Michel

IPC分类号： C07D209/30

CPC分类号： C07D471/04

摘要： L'invention a pour objet des dérivés d'indolizine de formule générale :

dans laquelle :
X représente un groupement -S ou -SO₂-,
R₁ et R₂, identiques ou différents, représentent chacun l'hydrogène,le radical méthyle ou éthyle ou un atome d'halogène,
R₃ représente l'hydrogène ou un radical alkyle en C₁-C₄,
R₄ représente un radical précurseur d'un groupement carboxy,
R représente un radical alkyle en C₁-C₆, cycloalkyle en C₃-C₆, ou phényle ainsi que leur utilisation en tant qu'intermédiaires pour la préparation de dérivés aminoalkoxybenzènesulfoxyl-indolizines pharmaceutiquement actifs.

摘要翻译： 本发明的主题是通式的中氮茚衍生物：其中：X darstellt到-S-或-SO 2 - 基团，R1和R2，相同或不同，各自代表氢，甲基或乙基基团或 卤原子，R3 darstellt氢或C1-C4烷基，R 4代表基团羧基的前体，R在制备药学上darstellt的C1-C6烷基，C3-C6环烷基或苯基基团，以及它们作为中间体 活性aminoalkoxybenzenesulphonylindolizine（aminoalkoxyphenylsulphonylindolizine）衍生物。

公开(公告)号：EP0563916A1

公开(公告)日：1993-10-06

申请号：EP93105332.6

申请日：1993-03-31

申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED

发明人： Kosley, Raymond W., Jr. ,  Flanagan, Denise M. ,  Martin, Lawrence Leo ,  Nemoto, Peter Allen

IPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/12 ,  C07D209/48 ,  A61K31/40

CPC分类号： C07D209/08 ,  A61K31/40 ,  C07D209/12 ,  C07D209/30

摘要： There are disclosed compounds having the formula

wherein

X is hydrogen, chloro, bromo, fluoro, hydroxy, loweralkoxy, arylloweralkoxy, acyloxy, loweralkylaminocarbonyloxy, diloweralkylaminocarbonyloxy, amino, loweralkylamino, diloweralkylamino, acylamino, loweralkyl or trifluoromethyl;
Y is hydrogen, loweralkyl, chloro or bromo;
Z is hydrogen, loweralkyl, loweralkoxy or halogen; or X and Z taken together can form a methylenedioxy group;
R¹ is hydrogen, loweralkyl, arylloweralkyl, carboxyloweralkyl, arylloweralkoxycarbonylloweralkyl or loweralkoxycarbonylloweralkyl;
R² is hydrogen, loweralkyl or hydroxyloweralkyl;
R³ is hydrogen or loweralkyl; or
R² and R³ together with the carbon to which they are attached form (C₃ - C₇)cycloalkyl;
R⁴ is hydrogen or loweralkyl;
R⁵ is hydrogen, loweralkyl, aryl, arylloweralkyl, acyl, arylloweralkoxycarbonyl, loweralkoxycarbonyl or aryloxycarbonyl;
R⁶ is hydrogen, chloro, bromo, arylcarbonyl, loweralkylcarbonyl, aryl(hydroxy)loweralkyl or hydroxyloweralkyl; and
m and n are independently 0 to 5 with the proviso that the sum of m plus n is not greater than 5;
and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and their use as neuroprotective agents.

摘要翻译： 有具有下式的游离缺失盘化合物 worin X是氢，氯，溴，氟，羟基，低级烷氧基，arylloweralkoxy，酰氧基，loweralkylaminocarbonyloxy，diloweralkylaminocarbonyloxy，氨基，低级烷基氨基，二低级烷氨基，酰氨基，低级烷基或三氟甲基; Y是氢，低级烷基，氯或溴; Z是氢，低级烷基，低级烷氧基或卤素; 或者X和可一起形成亚甲二基团Z; [R <1>是氢，低级烷基，芳基低级烷基，carboxyloweralkyl，arylloweralkoxycarbonylloweralkyl或loweralkoxycarbonylloweralkyl; [R <2>是氢，低级烷基或hydroxyloweralkyl; [R <3>是氢或低级烷基; 或R <2>和R <3>使用的碳原子一起与它们所连接形式（C3 - C7）环烷基; [R <4>是氢或低级烷基; [R <5>是氢，低级烷基，芳基，芳基低级烷基，酰基，arylloweralkoxycarbonyl，低级烷氧基羰或芳氧基羰基; [R <6>是氢，氯，溴，芳基羰基，loweralkylcarbonyl，芳基（羟基）低级烷基或hydroxyloweralkyl; 并且m和n是unabhängig0-5，条件做m的总和加上n是不大于5; 以及它们的药学上可接受的加成盐，或在适用情况下，光学或几何异构体或外消旋混合物，制备该化合物的，用于制备所述化合物和药物组合物及其作为神经保护剂使用的处理过程的中间体。

公开(公告)号：EP0556949A2

公开(公告)日：1993-08-25

申请号：EP93300225.5

申请日：1993-01-14

申请人： MARINE BIOTECHNOLOGY INSTITUTE CO., LTD.

发明人： Konya, Kazumi, c/o Shimizu Lab., Marine ,  Shimizu, Nobuyoshi, c/o Shimizu Lab., Marine ,  Miki, Wataru, c/o Shimizu Lab., Marine

IPC分类号： A01N43/38 ,  C09D5/14 ,  C07D209/30

CPC分类号： C09D5/1625 ,  A01N43/38 ,  A01N43/40 ,  C07D209/30

摘要： The present invention provides the use as undersea anti-fouling reagent of an indole compound of Formula (1):

(wherein Y represents hydrogen, lower alkyl, or phenyl; X¹, X², X³, X⁴, X⁵ and X⁶ independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, cyano, cyano lower alkyl, halogenated lower alkyl, di-lower-alkylamino-lower alkyl, etc.) The compounds of formula (1) are safe and effective underwater anti-fouling reagents.

摘要翻译： 本发明提供作为式（1）的吲哚化合物的海底防污试剂的用途：（其中Y表示氢，低级烷基或苯基; X 1，X 2，X 3 >，X 4，X 5和X 6独立地表示氢，卤素，低级烷基，低级烷氧基，硝基，氰基，氰基低级烷基，卤代低级烷基，二低级烷基氨基 - 低级烷基等 。）式（1）化合物是安全有效的水下防污试剂。

公开(公告)号：EP0525472A3

公开(公告)日：1993-02-24

申请号：EP92111757.8

申请日：1992-07-10

申请人： PHARMACIA S.p.A.

发明人： Buzzetti, Franco ,  Longo, Antonio ,  Colombo, Maristella

IPC分类号： C07D403/06 ,  C07D209/30 ,  A61K31/40 ,  A61K31/405

CPC分类号： C07D209/34

摘要： The invention provides new methylen-indole derivatives of formula (I)

wherein
R is a group

in which R 4 is hydrogen, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 alkanoyloxy, carboxy, nitro or NHR 7 , wherein R 7 is hydrogen or C 1 -C 6 alkyl; R 5 is hydrogen, C 1 -C 6 alkyl or halogen; and R 6 is hydrogen or C 1 -C 6 alkyl; n is zero, 1 or 2; R 1 is hydrogen, C 1 -C 6 alkyl or C 2 -C 6 alkanoyl; R 2 is hydrogen, C 1 -C 6 alkyl, halogen, cyano, carboxyl, nitro or -NHR 7 in which R 7 is as defined above; R 3 is hydrogen, C 1 -C 6 alkyl or C 2 -C 6 alkanoyl; and
the pharmaceutically acceptable salts thereof; and wherein, when,at the same time, R 2 is hydrogen, C 1 -C 6 alkyl, halogen or cyano and R 3 is hydrogen, R 1 and n being as defined above, then at least one of R 4 , R 5 and R 6 is other than hydrogen, which are useful as tyrosine kinase inhibitors.

公开(公告)号：EP0470665A1

公开(公告)日：1992-02-12

申请号：EP91201994.0

申请日：1991-08-01

申请人： EASTMAN KODAK COMPANY

发明人： Schleigh, William Robert, c/o Eastman Kodak Co. ,  Welter, Thomas Robert, c/o Eastman Kodak Co.

IPC分类号： A01N43/38 ,  A01N43/40 ,  C07D209/42 ,  C07D209/30

CPC分类号： C07D401/04 ,  A01N43/38 ,  A01N43/40 ,  C07D209/08 ,  C07D209/10 ,  C07D209/42 ,  C07D405/04

摘要： 1-Hydroxyindoles of the following formula are useful in controlling fungi:
wherein:

R 1 is hydrogen or an electron withdrawing group;
R 2 is selected from the group consisting of alkenyl having 2-10 carbon atoms, N-substituted-a-iminobenzyl,an unsubstituted or substituted aromatic group and acyl of 2-16 carbon atoms,
R 3 is selected from the group consisting of halogen atoms, and
n is 0 to 4.

摘要翻译： 下式的1-羟基吲哚可用于控制真菌：其中：R 1是氢或吸电子基团; R 2选自具有2-10个碳原子的烯基，N-取代-α-亚氨基苄基，未取代或取代的芳族基团和2-16个碳原子的酰基，R 3选自 卤素原子组成，n为0〜4

公开(公告)号：EP0429257A2

公开(公告)日：1991-05-29

申请号：EP90312489.9

申请日：1990-11-16

申请人： GLAXO GROUP LIMITED

发明人： Ross, Barry Clive ,  Middlemiss, David ,  Scopes, David Ian Carter ,  Jack, Torquil Iain Maclean ,  Cardwell, Kevin Stuart ,  Dowle, Michael Dennis

IPC分类号： C07D403/06 ,  C07D403/14 ,  C07D521/00 ,  A61K31/415 ,  C07D209/30

CPC分类号： C07D249/08 ,  C07D209/10 ,  C07D209/26 ,  C07D209/30 ,  C07D231/12 ,  C07D233/56 ,  C07D403/06 ,  C07D403/14

摘要： The invention provides compounds of the general formula (I):

or a physiologically acceptable salt or a solvate (e.g. hydrates) thereof in which
R¹ represents a hydrogen atom or a halogen atom or a group selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, fluoroC₁₋₆alkyl, -CHO, -CO₂H or -COR⁴;
R² represents a hydrogen atom or a halogen atom or the group Ar;
R³ represents a hydrogen atom or a group selected from C₁₋₆ alkyl, C₃₋₆alkenyl, C₁₋₆alkoxy, -COR⁴, -SO₂R⁴ or the group Ar;
R⁴ represents a group selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₁₋₆ alkoxy or the group -NR¹²R¹³;
Ar represents the group

R⁵ represents a group selected from -CO₂H, -NHSO₂CF₃ or a C-linked tetrazolyl group;
R⁶ and R⁷ which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C₁₋₆alkyl group;
Het represents an N-linked imidazolyl group substituted at the 2-position by a C₁₋₆alkyl, C₂₋₆alkenyl or a C₁₋₆alkylthio group, the imidazolyl group optionally being substituted by one or two further substituents selected from a halogen atom or a group selected from cyano, nitro, C₁₋₆alkyl, C₂₋₆alkenyl, fluoroC₁₋₆alkyl, -(CH₂) m R⁸, -(CH₂) n COR⁹, or -(CH₂) p NR¹⁰COR¹¹;
or Het represents an N-linked benzimidazolyl group substituted at the 2-position by a C₁₋₆alkyl, C₂₋₆alkenyl or a C₁₋₆alkylthio group;
R⁸ represents a hydroxy or C₁₋₆alkoxy group;
R⁹ represents a hydrogen atom or a group selected from hydroxy, C₁₋₆alkyl, C₁₋₆alkoxy, phenyl, phenoxy or the group -NR¹²R¹³;
R¹⁰ represents a hydrogen atom or a C₁₋₆alkyl group;
R¹¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₁₋₆alkoxy, phenyl, phenoxy or the group -NR¹²R¹³;
R¹² and R¹³ which may be the same or different each independently represent a hydrogen atom or a C₁₋₄alkyl group or -NR¹²R¹³ forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom;
m represents an integer from 1 to 4;
n represents an integer from 0 to 4; and
p represents an integer from 1 to 4;
provided that one of R² and R³ represents the group Ar, and that when R² represents the group Ar, R³ represents a hydrogen atom or a group selected from C₁₋₆ alkyl, C₃₋₆ alkenyl, C₁₋₆alkoxy -COR⁴ or -SO₂R⁴, and that when R³ represents the group Ar, R² represents a hydrogen atom or a halogen atom.
The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

摘要翻译： 本发明提供通式（I）的化合物：其中R 1表示氢原子或卤素原子或选自C 1-6的基团的生理学上可接受的盐或其溶剂合物（例如水合物） 烷基，C 2-6烯基，氟C 1-6烷基，-CHO，-CO 2 H或-COR 4; R 2表示氢原子或卤素原子或Ar基团; R 3表示氢原子或选自C 1-6烷基，C 3-6烯基，C 1-6烷氧基，-COR 4，-SO 2 R 4或基团Ar的基团; R 4表示选自C 1-6烷基，C 2-6烯基，C 1-6烷氧基或基团-NR 1 2 R 1 3的基团。 Ar表示基团 R 5表示选自-CO 2 H，-NHSO 2 CF 3或C连接的四唑基的基团; R 6和R 7可以相同或不同，各自独立地表示氢原子或卤素原子或C1-6烷基; Het表示在2-位被C 1-6烷基，C 2-6烯基或C 1-6烷硫基取代的N-连接的咪唑基，咪唑基任选被一个或两个选自卤素原子或基团的其它取代基取代 选自氰基，硝基，C 1-6烷基，C 2-6烯基，氟C 1-6烷基， - （CH 2）m R 8， - （CH 2）n COR 9或 - （CH 2）p NR R' 1> <1>; 或Het表示在2-位被C 1-6烷基，C 2-6烯基或C 1-6烷硫基取代的N-连接的苯并咪唑基; R 8表示羟基或C 1-6烷氧基; R 9表示氢原子或选自羟基，C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 1 2 R 1 3的基团。 R 1表示氢原子或C 1-6烷基; R 1表示氢原子或选自C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 1 R 2 3的基团。 R 1，R 2和R 3可以相同或不同，各自独立地表示氢原子或C 1-4烷基或-NR 1 2 R 1 3 形成饱和杂环，其具有5或6个环成员，并且可以任选地在环中含有一个氧原子; m表示1〜4的整数， n表示0〜4的整数， p表示1〜4的整数， 条件是R 2和R 3中的一个表示基团Ar，当R 2表示基团Ar时，R 3表示氢原子或选自C 1-6烷基， 6烯基，C 1-6烷氧基-COR 4或-SO 2 R 4，当R 3表示基团Ar时，R 2表示氢原子或卤素原子。 该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。