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    IMPROVED SYNTHESIS OF NICKEL PHOSPHINE AND PHOSPHITE CATALYSTS
    3.
    发明申请
    IMPROVED SYNTHESIS OF NICKEL PHOSPHINE AND PHOSPHITE CATALYSTS 审中-公开
    改善镍磷酸盐和磷酸盐催化剂的合成

    公开(公告)号：WO9511077A3

    公开(公告)日：1995-08-03

    申请号：PCT/US9411045

    申请日：1994-10-06

    Applicant: DU PONT

    Inventor： BRYNDZA HENRY E

    IPC: B01J31/18 ,  B01J31/24 ,  B01J37/34 ,  C07F9/141 ,  C07F15/04 ,  B01J

    CPC classification number: C07F15/04 ,  B01J31/185 ,  B01J31/1895 ,  B01J31/24 ,  B01J37/344 ,  B01J2231/323 ,  B01J2531/847 ,  C07F9/141

    Abstract: An improved process for the synthesis of zerovalent nickel catalyst useful for the hydrocyanation of olefins, wherein catalyst formation is improved by applying sonication during formation of catalyst. The sonication may be applied to the catalyst reactant mixture containing elemental nickel and a ligand; or alternatively, the sonication may be applied to the elemental nickel prior to the addition of ligand to the reaction mixture.

    Abstract translation: 用于合成可用于烯烃氢化氰化的零价镍催化剂的改进方法，其中通过在催化剂形成期间应用超声处理来改善催化剂形成。 超声处理可以应用于含有元素镍和配体的催化剂反应物混合物; 或者，在将配体加入到反应混合物之前，可以将超声处理施加到元素镍上。

    PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME
    4.
    发明申请
    PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME 审中-公开
    磷酸盐 - 硼烷化合物，以及制备和使用它们的方法

    公开(公告)号：WO1992020650A2

    公开(公告)日：1992-11-26

    申请号：PCT/US1992003833

    申请日：1992-05-08

    Applicant: BORON BIOLOGICALS, INC.

    Inventor： BORON BIOLOGICALS, INC. ,  SPIELVOGEL, Bernard, F. ,  SOOP, Anup ,  HALL, Iris, H.

    IPC: A61K31/69

    CPC classification number: C07H23/00 ,  C07F9/141 ,  C07F9/1415

    Abstract: Phosphite-borane compounds of formula (I) wherein each R1 is independently selected from: H; C1-C10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R4)4N+, in which the substituents R¿4? of the ammonium nitrogen atom are H or C1-C10 alkyl; R2 is H or C1-C10 alkyl; and R3 is CNCH2CH3?+BF¿4-, COOH, carboxyl salts, COOR¿5?, or CONHR5, wherein R5 is C1-C10 alkyl, alkylaryl, aralkyl, or aryl; with the proviso that if at least one of the R1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R3 may also be CN. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity. Also disclosed are various synthetic methods for making such phosphorous-boron compounds, and for formulating same in unit dosage forms as well as other pharmaceutically and pharmacologically acceptable formulations.

    COMPOSITIONS FOR TREATMENT OF INFLAMMATION-RELATED DISORDERS, PAIN AND FEVER, SKIN DISORDERS, CANCER AND PRECANCEROUS CONDITIONS THEREOF
    6.
    发明申请
    COMPOSITIONS FOR TREATMENT OF INFLAMMATION-RELATED DISORDERS, PAIN AND FEVER, SKIN DISORDERS, CANCER AND PRECANCEROUS CONDITIONS THEREOF 审中-公开
    用于治疗与感染相关的疾病，疼痛和感冒，皮肤疾病，癌症和预防性疾病的组合物

    公开(公告)号：WO2014047592A3

    公开(公告)日：2015-07-23

    申请号：PCT/US2013061247

    申请日：2013-09-23

    Applicant: RIGAS BASIL

    Inventor： RIGAS BASIL

    IPC: C07D475/00 ,  A61K31/60 ,  A61P29/00

    CPC classification number: C07F9/5728 ,  A61K45/06 ,  C07C233/54 ,  C07C235/64 ,  C07C235/84 ,  C07C237/42 ,  C07C327/32 ,  C07D209/26 ,  C07D451/14 ,  C07D475/04 ,  C07D493/20 ,  C07F9/091 ,  C07F9/093 ,  C07F9/094 ,  C07F9/141 ,  C07F9/6561 ,  C07F9/65742

    Abstract: The present invention provides novel compounds and pharmaceutical compositions suitable for administration to mammals, for the prevention and/or treatment of cancer, precancerous conditions, pain, fever, skin disorders, inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. These comprise a biologically active moiety or portion (A) preferably derived from a non-steroidal anti-inflammatory drug or NSAID (A), bound via a linker moiety (B) to functional moiety Z, which facilitates access of the compound into cells. The moiety Z can comprise, for example, a phosphorous-containing group, a nitrogen-containing group, or a folic acid residue.

    Abstract translation: 本发明提供适用于哺乳动物施用，用于预防和/或治疗癌症，癌前病症，疼痛，发热，皮肤病症，炎症相关疾病和/或心血管疾病的新型化合物和药物组合物。 本发明的化合物具有改善的功效和安全性，包括比常规疗法更高的效力和/或更少或更少的副作用。 它们包括生物活性部分或部分（A），优选衍生自通过接头部分（B）与功能部分Z结合的非甾体抗炎药或NSAID（A），其有助于化合物进入细胞。 部分Z可以包括例如含磷基团，含氮基团或叶酸残基。

    METHOD FOR PRODUCING ORGANOPHOSPHITES
    7.
    发明申请
    METHOD FOR PRODUCING ORGANOPHOSPHITES 审中-公开
    用于生产有机亚磷酸酯

    公开(公告)号：WO01032666A1

    公开(公告)日：2001-05-10

    申请号：PCT/EP2000/010520

    申请日：2000-10-25

    IPC: C07F9/141 ,  C07F9/145 ,  C07F9/146 ,  C07F9/48

    CPC classification number: C07F9/146 ,  C07F9/141 ,  C07F9/145

    Abstract: The invention relates to a method for producing compounds of formula X(1-a) R a P (OR )2 (I) or X(2-a) R a P (OR ) (II), wherein X: Cl, Br, J; R : an organic radical; R : an organic radical; and a: 0.1, characterised in that a) a compound (III) of formula PX(3-a)R a is reacted with a compound (IV) of formula R OH at temperatures of 10 to 200 DEG C, the molar ratio of the X radicals used to compound (IV) being 1:10 to 10:1, to obtain a mixture (V) containing compound (I) and compound (II), b) compounds (I) and (II) are separated from the mixture (V) and c) compound (I) or compound (II) is returned to step (a).

    Abstract translation: 一种用于式X的化合物的制备方法（1-A）R <2>一个P（OR <1>）2（I），或X（2-A）R <2>一个P（OR <1>）（II ）其中：X：氯，溴，J; [R <1>：有机基; [R <2>：有机基; A：0.1; 其特征在于该式PX（3-A）R <2>一与化合物（IV）式R a的）的化合物反应（III）<1> OH，在温度从10至200℃范围C， 其中X的摩尔比用于化合物（IV）为1:10至10：1，得到含有化合物（I）UDN化合物（II），b）从所述混合物（V），该化合物的混合物（V） （I）UDN（II）被分离出来和c）的化合物（I）或者在步骤（II）化合物（a）中引回。

    PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME
    9.
    发明申请
    PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME 审中-公开
    磷酸盐 - 硼烷化合物，以及制备和使用它们的方法

    公开(公告)号：WO9220650A3

    公开(公告)日：1993-03-04

    申请号：PCT/US9203833

    申请日：1992-05-08

    Applicant: BORON BIOLOG INC

    Inventor： SPIELVOGEL BERNARD F ,  SOOP ANUP ,  HALL IRIS H

    IPC: A61K31/69 ,  A61K31/70 ,  A61K31/7135 ,  A61P3/06 ,  A61P29/00 ,  A61P35/00 ,  C07F9/06 ,  C07F9/141 ,  C07F19/00 ,  C07H23/00 ,  C07F9/142 ,  C07H19/10 ,  C07H19/20

    CPC classification number: C07H23/00 ,  C07F9/141 ,  C07F9/1415

    Abstract: Phosphite-borane compounds of formula (I) wherein each R1 is independently selected from: H; C1-C10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R4)4N+, in which the substituents R¿4? of the ammonium nitrogen atom are H or C1-C10 alkyl; R2 is H or C1-C10 alkyl; and R3 is CNCH2CH3?+BF¿4-, COOH, carboxyl salts, COOR¿5?, or CONHR5, wherein R5 is C1-C10 alkyl, alkylaryl, aralkyl, or aryl; with the proviso that if at least one of the R1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R3 may also be CN. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity. Also disclosed are various synthetic methods for making such phosphorous-boron compounds, and for formulating same in unit dosage forms as well as other pharmaceutically and pharmacologically acceptable formulations.

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