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    PROCESS FOR THE SYNTHESIS OF N-(4-CYANO-3-TRIFLUOROMETHYLPHENYL)-3-(4-FLUOROPHENYL-SULFONYL)-2-HYDROXY-2-METHYL-PROPIONAMIDE
    22.
    发明申请
    PROCESS FOR THE SYNTHESIS OF N-(4-CYANO-3-TRIFLUOROMETHYLPHENYL)-3-(4-FLUOROPHENYL-SULFONYL)-2-HYDROXY-2-METHYL-PROPIONAMIDE 审中-公开
    合成N-（4-氰基-3-三氟甲基苯基）-3-（4-氟亚甲基 - 磺酰基）-2-羟基-2-甲基丙酰胺的方法

    公开(公告)号：WO01000608A1

    公开(公告)日：2001-01-04

    申请号：PCT/HU2000/000049

    申请日：2000-05-26

    IPC分类号： C07C253/30 ,  C07C255/60 ,  C07C303/28 ,  C07C309/66 ,  C07C315/02 ,  C07C317/46 ,  C07C319/14 ,  C07C323/60 ,  C07D327/10

    CPC分类号： C07C253/30 ,  C07C303/28 ,  C07C315/02 ,  C07C319/14 ,  C07D327/10 ,  C07C317/46 ,  C07C255/60 ,  C07C309/66 ,  C07C323/60

    摘要： Racemic or optically pure N-(4-cyano-3-trifluoromethylphenyl)-3-(4 -fluorophenylsulphonyl)-2-hydroxy-2-methylpropionamide of formula (I) is prepared by the following process: 2,3-dihydroxy-2-methylpropionic acid of formula (VII) is reacted with thionyl chloride to form 4-chlorocarbonyl-4-methyl-1,3,2-dioxathiolane-2-one of formula (VI), which is reacted with 4-cyano-3-trifluoromethylaniline. The resulting 4-{[4-cyano-3-(trifluoromethyl)anilino]carbonyl}-4-methyl-1,3,2-dioxat hiolane-2-one of formula (V) is hydrolysed to form N-[4-cyano-3-(trilfuoromethyl)phenyl]-2,3-dihydroxy-2-methylpropionamide of formula (IV), which is sulfonylated with a sulfonyl halogenide of formula R-SO2-X, in a halogenated hydrocarbon solvent in the presence of a tertiary amine base. The sulphonic ester derivative of formula (III) obtained is reacted with 4-fluorothiophenol in the presence of a base to give a thioether of formula (II) which is oxidized using an inorganic peroxy compound or aqueous hydrogen peroxide.

    摘要翻译： 通过以下方法制备式（I）的外消旋或光学纯的N-（4-氰基-3-三氟甲基苯基）-3-（4-氟苯基磺酰基）-2-羟基-2-甲基丙酰胺：2,3-二羟基-2 式（Ⅶ）的甲基丙酸与亚硫酰氯反应，形成式（Ⅵ）的4-氯羰基-4-甲基-1,3,2-二氧硫杂环戊烷-2-酮，其与4-氰基-3- 三氟甲基苯胺。 将所得的式（V）的4 - {[4-氰基-3-（三氟甲基）苯胺基]羰基} -4-甲基-1,3,2-二氧杂环己烷-2-酮水解，形成N- [4- （Ⅳ）的3-氰基-3-（三氟甲酰基）苯基] -2,3-二羟基-2-甲基丙酰胺，其在卤代烃溶剂中在式 叔胺碱。 得到的式（III）的磺酸酯衍生物与4-氟苯硫酚在碱的存在下反应，得到使用无机过氧化合物或过氧化氢水溶液氧化的式（II）的硫醚。

    NON-STEROIDAL AGONIST COMPOUNDS AND THEIR USE IN MALE HORMONE THERAPY
    25.
    发明申请
    NON-STEROIDAL AGONIST COMPOUNDS AND THEIR USE IN MALE HORMONE THERAPY 审中-公开
    非甾体激素化合物及其在雄性激素治疗中的用途

    公开(公告)号：WO98053826A1

    公开(公告)日：1998-12-03

    申请号：PCT/US1998/011020

    申请日：1998-05-29

    IPC分类号： A61K31/167 ,  A61K31/277 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46 ,  C07C323/60 ,  A61K31/505 ,  A61K31/165 ,  A61K31/22 ,  A61K31/275 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40 ,  A61K31/405 ,  A61K31/415 ,  A61K31/44 ,  A61K31/47

    CPC分类号： C07C323/60 ,  A61K31/167 ,  A61K31/277 ,  C07C235/16 ,  C07C255/60 ,  C07C317/46

    摘要： The present invention relates to a non steroidal agonist compound having formula (I) where R1, R2, and R3 are the same or different and are a hydrogen, a nitro, a cyano, a carbamoyl, a halogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a beta -chloroethylamine; R4 is a hydrogen, an alkyl, or is joined to R5; R5 is a hydrogen, a hydroxy, an alkoxy, an acyloxy, an amino, an alkylamino, a halogen, an alkyl, a haloalkyl, or is joined to R4; R6 is a hydrogen, an alkyl, or a haloalkyl; A1 and A2 is the same or different, each is a direct link or an alkylene; X1 is a halogen, an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or an alkylene; R7 is a hydrogen, a halogen, an alkoxy, a haloalkoxy, an acyloxy, a haloacyloxy, an aryloxy, a thioalkyl, a thioaryl, an amino, an alkylimino, an alkylamido group, a haloalkylamido group, or a phenyl optionally substituted with a halogen, a nitro group, an alkyl, a haloalkyl, a cyano, a hydroxyl, a carboxylic group, an amino, an alkylamino group, a dialkylamino group, a bisalkylamino group, a haloalkylamino group, a dihaloalkylamino group, a bishaloalkylamino group, an acylamido group, a diacylamido group, an alkylacylamido group, a haloacylamido group, a bis(haloacyl)imido group, or an alkylhaloacylamido group. The present invention further relates to a method of producing the non-steroidal agonist compound, a composition containing the non-steroidal agonist compound, and methods of binding an androgen receptor, suppressing spermatogenesis, and providing hormonal therapy for androgen-dependent conditions.

    摘要翻译： 本发明涉及具有式（I）的非甾体激动剂化合物，其中R 1，R 2和R 3相同或不同，为氢，硝基，氰基，氨基甲酰基，卤素，全氟烷基，卤代烷基酰氨基， 异硫氰酸酯，叠氮化物，重氮羰基，取代的环氧乙烷或β-氯乙胺; R4是氢，烷基，或与R5连接; R5是氢，羟基，烷氧基，酰氧基，氨基，烷基氨基，卤素，烷基，卤代烷基，或与R4结合; R6是氢，烷基或卤代烷基; A1和A2相同或不同，各自为直链或亚烷基; X1是卤素，氧，硫，亚磺酰基，磺酰基，氨基，烷基亚氨基或亚烷基; R 7是氢，卤素，烷氧基，卤代烷氧基，酰氧基，卤代酰氧基，芳氧基，硫代烷基，硫代芳基，氨基，烷基亚氨基，烷基酰氨基，卤代烷基酰氨基或任选被 卤素，硝基，烷基，卤代烷基，氰基，羟基，羧基，氨基，烷基氨基，二烷基氨基，双烷基氨基，卤代烷基氨基，二卤代烷基氨基，二卤代烷基氨基，二卤代烷基氨基 酰基酰氨基，二酰基酰氨基，烷基酰氨基，卤代酰氨基，双（卤代酰基）亚氨基或烷基卤代酰胺基。 本发明还涉及一种制备非甾体激动剂化合物的方法，含有非甾体激动剂化合物的组合物，和结合雄激素受体的方法，抑制精子发生，并为雄激素依赖性条件提供激素疗法。

    DIAMINOCYCLOBUTENE-3,4-DIONES
    27.
    发明申请
    DIAMINOCYCLOBUTENE-3,4-DIONES 审中-公开
    DIAMINOCYCLOBUTENE -3,4-二酮

    公开(公告)号：WO1996015103A1

    公开(公告)日：1996-05-23

    申请号：PCT/US1995013125

    申请日：1995-10-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： AMERICAN HOME PRODUCTS CORPORATION ,  ANTANE, Madelene, Miyoko ,  BUTERA, John, Anthony ,  HIRTH, Bradford, Hammond ,  ANTANE, Schuyler, Adam

    IPC分类号： C07C255/60

    CPC分类号： C07D213/75 ,  C07C233/41 ,  C07C255/60 ,  C07C271/28 ,  C07C311/08 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/42 ,  C07D217/02

    摘要： The compound of formula (I), wherein R1 and R2 are, independent from each other, hydrogen, C1-10 straight chain alkyl, C1-10 branched alkyl, or C3-10 cyclic or bicyclic alkyl; R3 is an acyl substituent selected from the group consisting of formyl, alkanoyl of 2 to 7 carbon atoms, alkenoyl of 3 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms; A is selected from the group consisting of (a), wherein R4 is hydrogen, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-6 alkylamino, C2-12 dialkylamino, C1-6 alkylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, nitro, cyano, carboxyl; or, A is a phenyl group of formula (b), wherein R5 and R6, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, C1-6 alkylamino, C2-12 dialkylamino, sulfamyl, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, arylcarboxamido containing 7 to 13 carbon atoms, C2 to C6 alkanoyl, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

    摘要翻译： 式（I）化合物，其中R 1和R 2彼此独立地为氢，C 1-10直链烷基，C 1-10支链烷基或C 3-10环状或双环烷基; R3是选自甲酰基，2至7个碳原子的烷酰基，3至7个碳原子的烯酰基，1至7个碳原子的烷基磺酰基，7至12个碳原子的芳酰基，9至20个芳基烯酰基 6至12个碳原子的芳基磺酰基，8至12个碳原子的芳基烷酰基或7至12个碳原子的芳烷基磺酰基; A选自（a），其中R 4是氢，C 1-6烷基，C 1-6全氟烷基，C 1-6烷氧基，C 1-6全氟烷氧基，氨基，C 1-6烷基氨基，C 2-12二烷基氨基，C 1 -6-烷基磺酰氨基，含有2至7个碳原子的烷基羧酰胺基，硝基，氰基，羧基; 或者A是式（b）的苯基，其中R 5和R 6彼此独立地选自：氰基，硝基，氨基，C 1-6烷基，C 1-6全氟烷基，C 1-6烷氧基， C 1-6全氟烷氧基，C 1-6烷基氨基，C 12-12二烷基氨基，氨磺酰基，C 1-6烷基磺酰胺基，C 6-12芳基磺酰氨基，含2至7个碳原子的烷基羧酰胺基，含有7至13个碳原子的芳基羧酰胺基，C 2至C 6烷酰基， 6烷基磺酰基，C 1-6全氟烷基磺酰基，C 6-12芳基磺酰基，氯，溴，氟，碘，1-咪唑基，羧基或氢; 或其药学上可接受的盐是平滑肌松弛剂。

    신규 스퀘어아마이드 유도체 및 이의 용도
    28.
    发明申请
    신규 스퀘어아마이드 유도체 및 이의 용도 审中-公开

    公开(公告)号：WO2022255770A1

    公开(公告)日：2022-12-08

    申请号：PCT/KR2022/007722

    申请日：2022-05-31

    申请人： 부산대학교 산학협력단 ,  고신대학교 산학협력단

    发明人： 윤화영 ,  정지영 ,  곽진숙 ,  김민정 ,  김소영

    IPC分类号： C07C255/28 ,  C07C255/60 ,  C07C317/32 ,  C07C311/41 ,  A61K31/136 ,  A61K31/18 ,  A61P35/00

    摘要： 본 발명은 신규 스퀘어아마이드 유도체 및 이의 용도에 관한 것으로, 유레아 모핵의 화합물을 생물학적 동등체(bioisostere)인 스퀘어아마이드로 치환하는 전략으로 eIF2α 인산화 효능을 통한 항암 활성을 나타내는 신규 유도체를 제공한다. 스퀘어아마이드는 카보닐 기에 연결된 이중 결합을 지닌 특이적인 구조를 포함한다. 사각 고리의 스쿼레이트 환에 아민기를 지닌 전구체를 컨쥬게이트 첨가 반응으로 매개하여 스퀘어아마이드 구조를 만들 수 있다. 본 발명은 다양한 치환기를 지닌 아닐린 환을 스퀘어아마이드에 도입한 핵심 중간체를 효율적으로 구축하고, 이를 활용하여 반대편 질소에 페녹시사이클로헥실 구조를 도입한 유도체를 제공한다. 합성된 신규 유도체는 eIF2α 인산화 효과 및 인 비트로(in vitro)에서 암세포 증식 저해 활성을 보이므로, 대사항암제로서 활용될 수 있다.