利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

17 条记录 (耗时 0.013 秒)

    Liposome compositions
    1.
    发明授权
    Liposome compositions 失效
    脂质体组成

    公开(公告)号：US07208174B2

    公开(公告)日：2007-04-24

    申请号：US11011266

    申请日：2004-12-14

    申请人： Joerg Huwyler ,  Anita Schnyder

    发明人： Joerg Huwyler ,  Anita Schnyder

    IPC分类号： A61K8/14 ,  C07K16/00

    CPC分类号： A61K9/1271 ,  A61K47/6849 ,  A61K47/6913

    摘要： The present invention provides a non-covalent coupling method for the preparation of sterically stabilized lipsomes which may be used for targeted drug delivery, e.g., pegylated liposomes. The method simplifies the attachment of targeting vectors to sterically stabilized liposomes. The present invention also provides a liposome composition comprising a compound of the formula and a compound of the formula Z-Y, wherein Z is any compound capable of binding to a cellular receptor, and X and Y are compounds which can interact with each other non-convalently, and wherein the substituents n, F1 and F2 are as provided in the specification.

    摘要翻译： 本发明提供了用于制备空间稳定的lipomes的非共价偶联方法，其可用于靶向药物递送，例如聚乙二醇化脂质体。 该方法简化了靶向载体与空间稳定的脂质体的连接。 本发明还提供一种脂质体组合物，其包含下式的化合物和式ZY的化合物，其中Z是能够结合细胞受体的任何化合物，X和Y是可以互不相互作用的化合物 ，并且其中取代基n，F1和F2如说明书中所提供。

    Liposome compositions
    2.
    发明申请
    Liposome compositions 失效
    脂质体组成

    公开(公告)号：US20050152963A1

    公开(公告)日：2005-07-14

    申请号：US11011266

    申请日：2004-12-14

    申请人： Joerg Huwyler ,  Anita Schnyder

    发明人： Joerg Huwyler ,  Anita Schnyder

    IPC分类号： A61K9/127 ,  A61K39/395 ,  A61K47/48

    CPC分类号： A61K9/1271 ,  A61K47/6849 ,  A61K47/6913

    摘要： The present invention provides a non-covalent coupling method for the preparation of sterically stabilized lipsomes which may be used for targeted drug delivery, e.g., pegylated liposomes. The method simplifies the attachment of targeting vectors to sterically stabilized liposomes. The present invention also provides a liposome composition comprising a compound of the formula and a compound of the formula Z-Y, wherein Z is any compound capable of binding to a cellular receptor, and X and Y are compounds which can interact with each other non-convalently, and wherein the substituents n, F1 and F2 are as provided in the specification.

    摘要翻译： 本发明提供了用于制备空间稳定的lipomes的非共价偶联方法，其可用于靶向药物递送，例如聚乙二醇化脂质体。 该方法简化了靶向载体与空间稳定的脂质体的连接。 本发明还提供一种脂质体组合物，其包含下式的化合物和式ZY的化合物，其中Z是能够结合细胞受体的任何化合物，X和Y是可以互不相互作用的化合物 ，并且其中取代基n，F1和F2如说明书中所提供。

    Process for the preparation of 7-substituted 3-alkyl-3H-isobenzofuran-1-one derivatives
    3.
    发明授权
    Process for the preparation of 7-substituted 3-alkyl-3H-isobenzofuran-1-one derivatives 失效
    制备7-取代的3-烷基-3H-异苯并呋喃-1-酮衍生物的方法

    公开(公告)号：US07528266B2

    公开(公告)日：2009-05-05

    申请号：US11874965

    申请日：2007-10-19

    申请人： Anita Schnyder ,  Marco Passafaro ,  Thomas Rapold

    发明人： Anita Schnyder ,  Marco Passafaro ,  Thomas Rapold

    IPC分类号： C07D307/20

    CPC分类号： C07D307/88 ,  C07C63/70

    摘要： The present invention relates to a first compound having the formula wherein R is halogen, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8haloalkyl, aryl-C1-C8-alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R3 is C2-C5alkyl or C1-C5haloalkyl, or a salt thereof. The present invention is also directed to a second compound having the formula wherein R is fluorine, bromine, iodine, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8- haloalkyl, aryl-C1-C8alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, with the proviso that R1 is different from C1-C8 alkyl or aryl if X is S, R is different from iodine if R2 is methyl, and R is different from fluorine, bromine or iodine if R2 is hydrogen.

    摘要翻译： 本发明涉及具有下式的第一化合物其中R是卤素，R 1 S（O）n或（R 1）2 NC（X）O; R1是C1-C8烷基，C1-C8卤代烷基，芳基-C1-C8-烷基或芳基; n为0,1,2或3; X是O或S; R3为C2-C5烷基或C1-C5卤代烷基，或其盐。 本发明还涉及具有下式的第二化合物其中R是氟，溴，碘，R 1 S（O）n或（R 1）2 NC（X）O; R1是C1-C8烷基，C1-C8-卤代烷基，芳基-C1-C8烷基或芳基; n为0,1,2或3; X是O或S; 并且R 2是氢，C 1 -C 4烷基或C 1 -C 4卤代烷基，条件是如果X是S，R 1不同于C 1 -C 8烷基或芳基，如果R 2是甲基，则R不同于碘，R不同于氟，溴 或如果R2为氢，则为碘。

    Process for the preparation of 7-substituted 3-alkyl-3H-isobenzofuran-1-one derivatives
    4.
    发明授权
    Process for the preparation of 7-substituted 3-alkyl-3H-isobenzofuran-1-one derivatives 有权
    制备7-取代的3-烷基-3H-异苯并呋喃-1-酮衍生物的方法

    公开(公告)号：US07307175B2

    公开(公告)日：2007-12-11

    申请号：US10478020

    申请日：2002-05-21

    申请人： Anita Schnyder ,  Marco Passafaro ,  Thomas Rapold

    发明人： Anita Schnyder ,  Marco Passafaro ,  Thomas Rapold

    IPC分类号： C07D307/00

    CPC分类号： C07D307/88 ,  C07C63/70

    摘要： Process for the preparation of compounds of formula (I) wherein R is halogen, R1O1R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkly, aryl-C1-C8alkyl, C1-C8haloalkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, in which process, in a solvent, (1) an aniline derivative of formula (IV) wherein R is as defined above, and R3 is C1-C5alkyl or C1-C5haloalkyl, is diazotised in the presence of a mineral acid to form the corresponding diazonium salt of formul (II) wherein R and R3 are as defined above, Am− is an anion, and m is 1 or 2, (2) the resulting diazonium salt of formula (II) is carbonylated in the presence of a catalyst, CO and optionally a buffer, to form a benzoic acid derivative of formula (III) wherein R and R3 are as defined above, and (3) the benzoic acid derivative of formula (III) is then subjected to benzylic lactonisation in the ortho-position alkyl chain R3 in the presence of a free-radical initiator and a halogenating agent.

    摘要翻译： 制备式（I）化合物的方法，其中R是卤素，R 1，R 1，R 1，S（O） n或（R 1）2 NC（X）O; R 1是C 1 -C 8烷基，芳基-C 1 -C 8烷基， C 1 -C 8烷基，C 1 -C 8卤代烷基或芳基; n为0,1,2或3; X是O或S; R 2是氢，C 1 -C 4烷基或C 1 -C 4烷基， 其中在溶剂中，（1）式（Ⅳ）的苯胺衍生物，其中R如上定义，R 3是C 1 H 3 C 1 -C 5烷基或C 1 -C 5卤代烷基在无机酸存在下重氮化，形成相应的重氮盐 式（II）其中R和R 3如上所定义，A m - 是阴离子，m是1或2，（2）所得到的重氮盐 在催化剂CO和任选的缓冲剂存在下将式（II）羰基化以形成式（III）的苯甲酸衍生物，其中R和R 3如上定义，和（3 ）然后在自由基引发剂和卤化剂的存在下，在邻位烷基链R 3 3上对式（III）的苯甲酸衍生物进行苄基内酯化。

    PROCESS FOR THE PREPARATION OF 7-SUBSTITUTED 3-ALKYL-3H-ISOBENZOFURAN-1-ONE DERIVATIVES
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF 7-SUBSTITUTED 3-ALKYL-3H-ISOBENZOFURAN-1-ONE DERIVATIVES 审中-公开
    制备3-取代的3-烷基-3H-异苯并呋喃-1-酮衍生物的方法

    公开(公告)号：US20080108813A1

    公开(公告)日：2008-05-08

    申请号：US11875122

    申请日：2007-10-19

    申请人： Anita SCHNYDER ,  Marco PASSAFARO ,  Thomas RAPOLD

    发明人： Anita SCHNYDER ,  Marco PASSAFARO ,  Thomas RAPOLD

    IPC分类号： C07D239/60 ,  C07D307/87

    CPC分类号： C07D307/88 ,  C07C63/70

    摘要： The present invention relates a process for the preparation of a compound of formula Ia The process includes the step of reacting a first compound having the formula at elevated reaction temperature in the presence of sulfur in a nucleophilic aromatic substitution reaction with an alkali metal sulfide, disulfide or polysulfide of the formula M2Sq wherein R is halogen, R1SO2 or (R1)2NC(X)O; R1 is C1-C8alkyl, aryl-C1-C8alkyl, C1-C8-haloalkyl or aryl; R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, X is O or S; and wherein M is an alkali metal or hydrogen, and q is 1, 2 or a fractional number from 1 to 7,

    摘要翻译： 本发明涉及一种制备式Ia化合物的方法。该方法包括使具有下式的第一种具有式的第一化合物在硫的存在下在升高的反应温度下在亲核芳族取代反应中与碱金属硫化物，二硫化物 或多硫化物，其结构式为：α-in-line-formula description =“In-line Formulas”end =“lead”？> M -formulae description =“In-line Formulas”end =“tail”？>其中R是卤素，R 1 SO 2或（R 1）/ SO 2 2）NC（X）O; R 1是C 1 -C 8烷基，芳基-C 1 -C 8烷基， C 1 -C 6烷基，C 1 -C 8 - 卤代烷基或芳基; R 2是氢，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 卤代烷基，X是O或S; 并且其中M为碱金属或氢，q为1,2或1至7的分数，

    Microbiocidal N-phenyl-N-[4-(4-pyridyl-2-pyrimidin-2-yl]-amine derivatives
    7.
    发明授权
    Microbiocidal N-phenyl-N-[4-(4-pyridyl-2-pyrimidin-2-yl]-amine derivatives 失效

    公开(公告)号：US07074787B2

    公开(公告)日：2006-07-11

    申请号：US10451930

    申请日：2001-12-20

    申请人： Martin Eberle ,  Hugo Ziegler ,  Fredrik Cederbaum ,  Peter Ackermann ,  Anita Schnyder

    发明人： Martin Eberle ,  Hugo Ziegler ,  Fredrik Cederbaum ,  Peter Ackermann ,  Anita Schnyder

    IPC分类号： C07D401/04 ,  C07D413/04 ,  A01N43/54

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14

    摘要： The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (I) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1–C6-alkyl, C1–C6-haloalkyl or C1–C6-alkoxy; R2A is hydrogen, C1–C6-alkyl, C3–C4-alkenyl or C3–C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1–C6-alkyl, C1–C6-haloalkyl, hydroxy-C1–C6-alkyl or C1–C6-alkoxy-C1–C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C═O) or a group C═S; X is C═O, C═S, S═O or O═S═O; Y is O, S, C═O, CH2, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1–C4-alkyl, C3–C4-alkenyl, C3–C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8, SO2R8, SOR8 or SR8; and R8 is C1–C8-alkyl, C1–C8-alkoxyalkyl, C1–C8 haloalkyl or phenylC1–C2-alkyl wherein the phenyl may be substituted by up to three groups selected from halo or C1–C4-alkyl; or a salt thereof. The invention also relates to the preparation of the compounds and to agrochemical compositions comprising at least one of those compounds as active ingredient as well as the preparation of the said compositions and to the use of the compounds or of the compositions in controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.

    Process for the preparation of aromatic carboxylic acid amides
    8.
    发明授权
    Process for the preparation of aromatic carboxylic acid amides 失效
    芳香族羧酸酰胺的制备方法

    公开(公告)号：US06441233B1

    公开(公告)日：2002-08-27

    申请号：US09885103

    申请日：2001-06-21

    申请人： Anita Schnyder ,  Adriano Indolese ,  Gerald Mehltretter

    发明人： Anita Schnyder ,  Adriano Indolese ,  Gerald Mehltretter

    IPC分类号： C07C23110

    CPC分类号： C07C231/10 ,  C07D213/81

    摘要： A process for the preparation of primary aromatic carboxamides by the carbonylation of an aromatic compound, which contains at least one leaving group, with carbon monoxide, in the presence of a homogeneous or heterogeneous Pd catalyst and at least stoichiometric amounts of an amidation agent at elevated temperatures, which is characterized in that a primary carboxamide or a primary urethane is used as the amidation agent, and the reaction is carried out in the presence of an acylation catalyst.

    摘要翻译： 在均相或多相Pd催化剂存在下，通过羰基化含有至少一个离去基团的芳族化合物与一氧化碳来制备伯芳香族羧酰胺的方法，以及至少化学计量的酰胺化剂 温度，其特征在于使用初级羧酰胺或伯氨基甲酸酯作为酰胺化剂，反应在酰化催化剂存在下进行。

    Process
    10.
    发明授权
    Process 失效
    处理

    公开(公告)号：US5952524A

    公开(公告)日：1999-09-14

    申请号：US65270

    申请日：1998-04-23

    申请人： Victor Eliu ,  Werner Kanert ,  Adriano Indolese ,  Ian John Fletcher ,  Julia Volkel ,  Anita Schnyder

    发明人： Victor Eliu ,  Werner Kanert ,  Adriano Indolese ,  Ian John Fletcher ,  Julia Volkel ,  Anita Schnyder

    IPC分类号： B01J31/22 ,  C07B37/04 ,  C07B61/00 ,  C07C2/86 ,  C07C15/52 ,  C07C17/263 ,  C07C25/24 ,  C07C67/333 ,  C07C69/76 ,  C07C201/12 ,  C07C205/06 ,  C07C303/22 ,  C07C303/32 ,  C07C303/34 ,  C07C309/29 ,  C07C309/32 ,  C09B57/00 ,  C11D3/42 ,  C07C321/00

    CPC分类号： C07C303/32 ,  C07C303/22

    摘要： The present invention provides a process for the production of a compound of formula: ##STR1## in which X and Y, independently, are hydrogen, halogen, NO.sub.2, CF.sub.3, CN, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, COO--C.sub.1 -C.sub.4 alkyl, CO--C.sub.1 -C.sub.4 alkyl, NH--(C.sub.1 -C.sub.4 alkyl), N(C.sub.1 -C.sub.4 alkyl).sub.2, NH(C.sub.1 -C.sub.4 alkyl-OH), N(C.sub.1 -C.sub.4 alkyl-OH).sub.2, COOH or SO.sub.3 H or an ester or amide thereof, or COOM or SO.sub.3 M in which M is Na, K, Ca, Mg, ammonium, mono-, di-, tri- or tetra-C.sub.1 -C.sub.4 alkylammonium, mono-, di- or tri-hydroxyalkylammonium or ammonium that is di- or tri-substituted with a mixture of C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 hydroxyalkyl groups;Z is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, halogen (F, Cl, Br, I), SO.sub.3 H or SO.sub.3 M in which M has its previous significance; andn is 1 or 2; comprisingA) reacting a diazonium compound having the formula: ##STR2## in which X and n have their previous significance and G is a counter ion, with ethylene in the presence of an inorganic or organic palladium compound, or a mixture thereof, as catalyst-precursor, to produce a compound having the formula: ##STR3## in which X and n have their previous significance; and B) reacting 2 moles of the compound of formula (3) with 1 mole of a compound having the formula: ##STR4## In which Z has its previous significance and each R.sub.1 is the same and is a bromine or iodine atom, in the presence of an inorganic or organic palladium compound, or a mixture thereof, as catalyst-precursor, to produce a compound having the formula (1). The compounds of formula (1) are useful as fluorescent whitening agents.

    摘要翻译： 本发明提供一种制备下式化合物的方法：其中X和Y独立地是氢，卤素，NO 2，CF 3，CN，C 1 -C 4烷基，C 1 -C 4烷氧基，COO-C 1 -C 4烷基，CO- C 1 -C 4烷基，NH-（C 1 -C 4烷基），N（C 1 -C 4烷基）2，NH（C 1 -C 4烷基-OH），N（C 1 -C 4烷基-OH）2，COOH或SO 3 H或其酯或酰胺， COOM或SO 3 M，其中M是Na，K，Ca，Mg，铵，一，二，三或四-C 1 -C 4烷基铵，二 - 或三 - 被C1-C4烷基和C1-C4羟烷基的混合物取代; Z为氢，C1-C4烷基，C1-C4烷氧基，CF3，卤素（F，Cl，Br，I），SO3H或SO3M，其中M具有以前的意义; n为1或2; 包括：A）使无机或有机钯化合物或其混合物作为催化剂前体的具有下式的重氮化合物：其中X和n具有其先前的含义，G是抗衡离子，与乙烯反应， 以产生具有下式的化合物：其中X和n具有其先前的含义; 和B）使2摩尔式（3）化合物与1摩尔具有下式的化合物反应：其中Z具有其先前的含义，并且每个R 1相同且为溴或碘原子，在 无机或有机钯化合物或其混合物作为催化剂前体，以制备具有式（1）的化合物。 式（1）的化合物可用作荧光增白剂。