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    PROCESS FOR THE PREPARATION OF (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE
    14.
    发明公开
    PROCESS FOR THE PREPARATION OF (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE 审中-公开
    制备（1S，4S，5S）-4-溴-6-氧杂环十二烯[3.2.1]辛烷-7-酮的方法

    公开(公告)号：EP2922833A1

    公开(公告)日：2015-09-30

    申请号：EP13815595.7

    申请日：2013-11-22

    申请人： Daiichi Sankyo Co., Ltd.

    发明人： NAKAMURA, Yoshitaka ,  MUKESH, Kumar Madhra ,  INAMDAR, Murad Ismail

    IPC分类号： C07D307/94 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07C269/00 ,  C07D307/00 ,  C07D307/94

    摘要： The present invention relates to an improved and industrially advantageous process for the preparation of (1S, 4S, 5S) -4-bromo-6-oxabicyclo [3.2.1] octan-7-one represented by the following formula (I) which is a key intermediate in the synthesis of edoxaban, a compound that exhibits an inhibitory effect on activated blood coagulation factor X (also referred to as activated factor X or FXa), and is useful as a preventive and/or therapeutic drug for thrombotic diseases. The process includes reacting (1S) -cyclohex-3-ene-1-carboxylic acid of formula (II) with a brominating agent selected from the group consisting of N-bromosuccinimide or 1, 3-dibromo-5, 5-dimethylhydantoin in the presence of a base selected from calcium oxide or calcium hydroxide in a solvent selected from the group comprising of dichloromethane, toluene, tetrahydrofuran, ethy1 acetate, hexanes, cyclopentyl methyl ether (CPME) or a mixture thereof to get ( 1S, 4S, 5S) -4-bromo-6-oxabicyclo [3.2.1] octan-7-one of formula (I).

    摘要翻译： 本发明涉及用于制备由下式（I）表示的（1S，4S，5S）-4-溴-6-氧杂双环[3.2.1]辛烷-7-酮的工业上有利的方法，其为 它是合成依托沙班的关键中间体，对活化的血液凝固因子X（也称为活化的X因子或FXa）表现出抑制作用的化合物，可用作血栓性疾病的预防和/或治疗药物。 该方法包括使式（II）的（1S） - 环己-3-烯-1-羧酸与选自N-溴代琥珀酰亚胺或1,3-二溴-5,5-二甲基乙内酰脲的溴化剂在 在选自二氯甲烷，甲苯，四氢呋喃，乙酸乙酯，己烷，环戊基甲基醚（CPME）或其混合物的溶剂中选择氧化钙或氢氧化钙的碱以得到（1S，4S，5S） （I）的-4-溴-6-氧杂双环[3.2.1]辛烷-7-酮。

    THROMBOXANE LIGANDS
    18.
    发明公开
    THROMBOXANE LIGANDS 审中-公开
    血栓素配体

    公开(公告)号：EP1015443A1

    公开(公告)日：2000-07-05

    申请号：EP98944822.0

    申请日：1998-09-09

    申请人： Allergan Sales, Inc.

    发明人： BURK, Robert, M.

    IPC分类号： C07D319/08 ,  A61K31/335

    CPC分类号： C07D319/08 ,  A61K31/558 ,  C07D307/00 ,  C07D493/08

    摘要： A method of treating ocular hypotension, hypertension, hemorrhage, myocardial ischemia, angina pectoris, coronary contraction, cerebrovascular contraction after subarachnoidal hemorrhage, and asthma which comprises administering to a mammal suffering therefrom a therapeutically effective amount of a thromboxane ligand which is a compound of formula (I), wherein Y is (CH2)x; Z is selected fom the group consisting of (1) and (CR2)x, x is an integer of 1 or 2; R2 is hydrogen or an alkyl radical of from 1 to 4 carbons, A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups or said alkylene or alkenylene may have one or more enchained oxo or imino radicals; B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms, or substituted derivatives of said methyl, cycloalkyl or aryl radicals wherein said substituent is selected from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alklycarboxy; and X is selected from the group consisting of cyano, -COOR, -CH2OR, -C(O)N(R2), -CH2N(R2) -CH=N-OH AND -CH2SR1 radicals wherein R is hydrogen or a C1 to C10 alkyl, phenyl or benzyl and E is O or S; or a pharmaceutically acceptable salt thereof.

    7- CARBOXYALKYL OR ALKENYL]-6- ALKYL OR ALKENYL] 3-OXO-2,4-DIOXOBICYCLO- 3.2.1] OCTANE AND DERIVATIVES THEREOF
    20.
    发明公开
    7- CARBOXYALKYL OR ALKENYL]-6- ALKYL OR ALKENYL] 3-OXO-2,4-DIOXOBICYCLO- 3.2.1] OCTANE AND DERIVATIVES THEREOF 失效
    7-（羧基烷基或链烯基）-6-（烷基或烯基）-3-氧代-2,4- DIOXOBICYCLO-（3.2.1）辛烷及其衍生物

    公开(公告)号：EP0737185A1

    公开(公告)日：1996-10-16

    申请号：EP95904826.0

    申请日：1994-12-05

    申请人： Allergan

    发明人： BURK, Robert, M. ,  KRAUSS, Achim, H. ,  WOODWARD, David, F.

    IPC分类号： A61K31 ,  A61P27 ,  C07D307 ,  C07D319 ,  C07D493

    CPC分类号： C07D307/00 ,  C07D319/08 ,  C07D493/08

    摘要： The present invention relates to 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl]-3-oxo-2,4-dioxobicyclo[3.2.1] octanes and derivatives thereof. In particular, hydroxyl, nitro, amino, amido, azido, oxime, thiol, ether and thiol ether derivatives of said carboxy group are contemplated. In particular, 7-[6-carboxy-2-hexenyl]-6-[3-hydroxy-1-octenyl] of 3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof are disclosed. These compounds are useful as ocular hypotensives and as (a) thromboxane mimetics for the prevention of hemorrhaging as follows: during surgery; tooth extraction; hemorrhaging associated with gastro-intestinal diseases and conditions such as hemorrhoids, inflammatory bowel diseases and gastric and peptic ulcers; as a result of stroke; as a complication in retinal diseases resulting in impaired vision and associated with menstruation, childbirth and uterine dysfunction and (b) selective vasoconstrictors for treating systemic hypotension, e.g. in restoring normal blood pressure in hemorrhagic, anaphylactic, or septic shock victims; to provide local anti-inflammatory effects in the eye, skin and nose; to limit plasma exudation in burns, etc. and optimizing blood-born delivery of drugs and diagnostics in encapsulating vehicles.