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    METHODS FOR PREPARING PENAMS
    1.
    发明公开
    METHODS FOR PREPARING PENAMS 审中-公开
    PENAMS制备方法

    公开(公告)号：EP3231806A1

    公开(公告)日：2017-10-18

    申请号：EP17168966.4

    申请日：2015-05-14

    申请人： Allecra Therapeutics SAS

    发明人： FAINI, Andrea ,  FORZATTI, Marco ,  FOGLIATO, Giovanni ,  BIONDI, Stefano

    IPC分类号： C07D499/87

    CPC分类号： C07D499/87 ,  C07F7/1896 ,  Y02P20/55

    摘要： A method of forming a compound of formula (IV) comprising the step of reacting a compound of formula (III) with a 2-ethylhexanoate salt:

    wherein R 1 in each occurrence is independently selected from H, halogen, amino, C 1-5 alkyl, C 2-5 alkenyl and C 2-5 alkynyl; R 2 in each occurrence is independently selected from H, halogen, amino, C 1-5 alkyl, C 2-5 alkenyl and C 2-5 alkynyl; and R 4 is C 1-5 alkyl; X- is an anion and each R 3 is independently selected from the group consisting of C 1-10 hydrocarbyl and C 1-5 alkoxy.

    摘要翻译： 形成式（IV）化合物的方法包括使式（III）化合物与2-乙基己酸盐反应的步骤：其中R 1在每种情况下独立地选自H，卤素，氨基，C 1-5烷基， C2-5链烯基和C2-5炔基; R 2在每次出现时独立地选自H，卤素，氨基，C 1-5烷基，C 2-5烯基和C 2-5炔基; 和R4是C1-5烷基; X-是阴离子，每个R3独立地选自C1-10烃基和C1-5烷氧基。

    PENAM CRYSTAL AND PROCESS FOR PRODUCING THE SAME
    3.
    发明公开
    PENAM CRYSTAL AND PROCESS FOR PRODUCING THE SAME 有权
    PENAMKRISTALL和方法及其

    公开(公告)号：EP1671975A4

    公开(公告)日：2007-03-14

    申请号：EP04792516

    申请日：2004-10-08

    申请人： OTSUKA CHEMICAL CO LTD ,  TAIHO PHARMACEUTICAL CO LTD

    发明人： TOKUMARU YOSHIHISA ,  SHIMABAYASHI AKIHIRO

    IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/86 ,  C07D499/87 ,  C07D499/897

    CPC分类号： C07D499/86

    摘要： Novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam­-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in producing 2α-methyl-2β-[(1,2,3-triazol-1-yl)­methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing TMPB-acetone crystals which comprises (A) the step of concentrating an organic solvent solution containing TMPB, (B) the step of dissolving the resultant concentrate in acetone, and (C) the step of crystallizing TMPB-acetone crystals from the acetone solution obtained; and a process for producing TAZB which comprises the step of reacting TMPB-acetone crystals with an oxidizing agent.

    METHOD FOR PREPARING PENAMS
    6.
    发明授权
    METHOD FOR PREPARING PENAMS 有权

    公开(公告)号：EP3143028B1

    公开(公告)日：2018-09-26

    申请号：EP15726552.1

    申请日：2015-05-14

    申请人： Allecra Therapeutics SAS

    发明人： FAINI, Andrea ,  FORZATTI, Marco ,  FOGLIATO, Giovanni ,  BIONDI, Stefano

    IPC分类号： C07D499/87

    CPC分类号： C07D499/87 ,  C07F7/1896 ,  Y02P20/55

    摘要： A method of forming a compound of formula (IV) comprising the step of reacting a compound of formula (III) with a 2-ethylhexanoate salt: wherein R 1 in each occurrence is independently selected from H, halogen, amino, C 1-5 alkyl, C 2-5 alkenyl and C 2-5 alkynyl; R 2 in each occurrence is independently selected from H, halogen, amino, C 1-5 alkyl, C 2-5 alkenyl and C 2-5 alkynyl; and R 4 is C 1-5 alkyl; X- is an anion and each R 3 is independently selected from the group consisting of C 1-10 hydrocarbyl and C 1-5 alkoxy.

    METHOD FOR PREPARING PENAMS
    7.
    发明公开
    METHOD FOR PREPARING PENAMS 审中-公开
    VORRICHTUNG ZUR HERSTELLUNG VON PENAMEN

    公开(公告)号：EP3143028A2

    公开(公告)日：2017-03-22

    申请号：EP15726552.1

    申请日：2015-05-14

    申请人： Allecra Therapeutics SAS

    发明人： FAINI, Andrea ,  FORZATTI, Marco ,  FOGLIATO, Giovanni ,  BIONDI, Stefano

    IPC分类号： C07D499/87

    CPC分类号： C07D499/87 ,  Y02P20/55

    摘要： A method of forming a compound of formula (IV) comprising the step of reacting a compound of formula (III) with a 2-ethylhexanoate salt: wherein R 1 in each occurrence is independently selected from H, halogen, amino, C 1-5 alkyl, C 2-5 alkenyl and C 2-5 alkynyl; R 2 in each occurrence is independently selected from H, halogen, amino, C 1-5 alkyl, C 2-5 alkenyl and C 2-5 alkynyl; and R 4 is C 1-5 alkyl; X- is an anion and each R 3 is independently selected from the group consisting of C 1-10 hydrocarbyl and C 1-5 alkoxy.

    摘要翻译： 形成式（IIIa）化合物的方法; 其中：R 1在每次出现时独立地选自H，卤素，氨基，C 1-5烷基，C 1-5烯基和C 1-5炔基; R2各自独立地选自H，卤素，氨基，C 1-5烷基，C 1-5烯基和C 1-5炔基; R4是C1-5烷基; 并且R 6是C 1-5氟烷基; PG是保护基，该方法包括使式（Ⅰaa）化合物与式（Ⅷ）化合物反应的步骤。

    2-BETA-SUBSTITUTED-6-ALKYLIDENE PENICILLANIC ACID DERIVATIVES AS BETA-LACTAMASE INHIBITORS
    9.
    发明授权
    2-BETA-SUBSTITUTED-6-ALKYLIDENE PENICILLANIC ACID DERIVATIVES AS BETA-LACTAMASE INHIBITORS 有权
    2-β取代-6-ALKYLIDENPENIZILLANSÄURE衍生物作为β-内酰胺酶抑制剂

    公开(公告)号：EP0966471B1

    公开(公告)日：2002-06-12

    申请号：EP98964952.0

    申请日：1998-12-29

    申请人： Research Corporation Technologies, Inc

    发明人： BUYNAK, John, D. ,  RAO, Akireddy, Srinivasa ,  DOPPALAPUDI, Venkata Ramana

    IPC分类号： C07D499/87 ,  A61K31/43

    CPC分类号： C07D499/00

    摘要： Compounds of formula (I), wherein R?1 and R2¿ are each independently hydrogen, (C¿1?-C10)alkyl, (C3-C8)cycloalkyl, (C2-C10)alkenyl, (C2-C10)alkynyl, -COORa, -CONRbRc, cyano, -C(=O)Rd, -ORe, aryl, heteroaryl, oxazolidinyl, isoxazolidinyl, morpholinyl, -S(O)mRf, -NRgRh, azido, or halo; R?3¿ is (C¿3?-C10)alkyl, (C2-C10)alkenyl, (C2-C10)alkynyl, (C1-C10)alkanoyl, (C3-C8)cycloalkyl, aryl, heteroaryl, aryl(C1-C10)alkyl, heteroaryl(C1-C10)alkyl, or -CH2Ri, wherein Ri is halo, cyano, cyanato, -ORj, -NRkRl, azido, -SRm, or (C3-C8)cycloalkyl; R?4¿ is hydrogen, (C¿1?-C10)alkyl, (C3-C8)cycloalkyl, (C2-C10)alkenyl, (C2-C10)alkynyl, aryl, or heteroaryl; m and n are each independently 0, 1, or 2; and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), and novel intermediates useful for the synthesis of compounds of formula (I).

    PROCESS FOR PRODUCING EXO-METHYLENEPENAM COMPOUNDS
    10.
    发明公开
    PROCESS FOR PRODUCING EXO-METHYLENEPENAM COMPOUNDS 失效
    VERFAHREN ZUR HERSTELLUNG VON EXO-METHYLENPENAM-DERIVATEN

    公开(公告)号：EP0999213A4

    公开(公告)日：2000-05-10

    申请号：EP98905768

    申请日：1998-03-05

    申请人： OTSUKA KAGAKU KK

    发明人： TORII SIGERU ,  TANAKA HIDEO ,  KAMEYAMA YUTAKA ,  TOKUMARU YOSHIHISA

    IPC分类号： C07D499/00 ,  C07D499/06 ,  C07D499/46 ,  C07D499/87

    CPC分类号： C07D499/00

    摘要： A process for preparing an exo-methylenepenam compound represented by the formula (2) wherein cephem compound represented by the formula (1) is reduced with a metal having a standard oxidation-reduction potential of up to -0.3 (V/SCE) in an amount of at least one mole per mole of the cephem compound and with a metal compound having a higher standard oxidation reduction potential than the metal in an amount of 0.0001 to 10 moles per mole of the cephem compound to obtain the exo-methylenepenam compound wherein R is a hydrogen atom, amino or protected amino, R is a hydrogen atom, halogen atom, etc. R is a hydrogen atom or carboxylic acid protective group, X is a halogen atom, etc. wherein R , R and R are as defined above.d

    摘要翻译： 制备通式（2）的外型 - 亚甲基戊酰胺化合物的方法，其中R1代表氢原子，氨基或被保护的氨基; R2代表氢原子，卤素原子等; 和R 3代表氢原子或羧基保护基，其特征在于还原通式（1）的头孢烯化合物，其中R 1，R 2和R 3各自如上所定义; X表示卤素原子等，至少等摩尔量的标准氧化还原电位为-0.3（V / SCE）以下的金属和0.0001〜30摩尔每摩尔化合物的 具有比金属高的标准氧化还原电位的金属化合物。