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    Pyrimidine derivatives as selective inhibitors of COX-2
    1.
    发明授权
    Pyrimidine derivatives as selective inhibitors of COX-2 失效
    嘧啶衍生物作为COX-2的选择性抑制剂

    公开(公告)号：US06780870B2

    公开(公告)日：2004-08-24

    申请号：US10182788

    申请日：2002-07-31

    申请人： Malcolm Clive Carter ,  Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Malcolm Clive Carter ,  Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    IPC分类号： C07D23942

    CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R1 and R2 are independently selected from H, or C1-6alkyl; R3 is C1-6alkyl or NH2; R4 is H or C1-6alkyl; A is a 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R5; R5 is halogen, C1-6alkyl, C1-6alkyl substituted by one ore more F, C1-6alkoxy, C1-6alkoxy substituted by one or more F, SO2NH2 or SO2C1-6alkyl; and n is 1 to 4.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 1和R 2独立地选自H或C 1-6烷基; R 3是C 1-6烷基或NH 2; R 4是H或C 1-6烷基; A是5或6元芳基或被一个或多个R 5取代的5或6元芳基; R 5是卤素，C 1 -C 6烷基， 被一个或多个F，C 1-6烷氧基，被一个或多个F，SO 2 NH 2或SO 2 C 1-6烷基取代的C 1-6烷氧基取代的C 1-6烷基; andn是1到4。

    Process for the preparation of N-(amino-4, 6-dihalo-pyrimidine) formamides
    2.
    发明授权
    Process for the preparation of N-(amino-4, 6-dihalo-pyrimidine) formamides 失效
    制备N-（氨基-4,6-二卤代 - 嘧啶）甲酰胺的方法

    公开(公告)号：US06716981B2

    公开(公告)日：2004-04-06

    申请号：US09867552

    申请日：2001-05-31

    申请人： Elie Saikali ,  Walter Brieden

    发明人： Elie Saikali ,  Walter Brieden

    IPC分类号： C07D23942

    CPC分类号： C07D239/48

    摘要： A process for the preparation of a 2,5-diamino-4,6-dihalopyrimidine of the formula: in which X is a halogen atom, comprising reacting 2,5-diamino-4,6-dihydroxypyrimidine or its salt of the formula: with a phosphorus oxyhalide and a quaternary ammonium halide or an amine in a halogenated hydrocarbon as a solvent.

    摘要翻译： 一种制备下式的2,5-二氨基-4,6-二卤代嘧啶的方法，其中X是卤素原子，包括使2,5-二氨基-4,6-二羟基嘧啶或其下式的盐： 在卤代烃中作为溶剂使用卤氧化磷和季铵卤化物或胺。

    Preparation of 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester
    3.
    发明授权
    Preparation of 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester 有权
    制备4-（4-氟苯基）-6-烷基-2-N-烷烃磺酰基-N-烷基氨基）嘧啶-5-甲酸酯

    公开(公告)号：US06710178B2

    公开(公告)日：2004-03-23

    申请号：US10443797

    申请日：2003-05-23

    申请人： Ulrich Veith

    发明人： Ulrich Veith

    IPC分类号： C07D23942

    CPC分类号： C07D239/42 ,  C07C229/34 ,  C07C311/05

    摘要： A process for the preparation of a 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester of formula (Ib), in which R1, R2, R3 and R4 are identical or different and are each a C1-6-alkyl. A 2-[-1-amino-1-(4-flourophenyl)methylene]-4-alkyl-3-oxo-alkanoic acid ester of formula (IIIb), in which R3 and R4 have the above-mentioned meanings, is reacted with an N-cyano-N-alkylalkanesulfonamide, optionally isolated or prepares in situ, of formula (IVb), in which R1 and R2 have the above-mentioned meanings, to give the final product of formula (Ib).

    摘要翻译： 制备式（Ib）的4-（4-氟苯基）-6-烷基-2-N-烷基磺酰基-N-烷基氨基）嘧啶-5-甲酸酯的方法，其中R 1，R R 2，R 3和R 4相同或不同，各自为C 1-6 - 烷基。 式（IIIb）的2 - [ - 1-氨基-1-（4-氟苯基）亚甲基] -4-烷基-3-氧代 - 链烷酸酯，其中R 3和R 4具有上述 与式（Ⅳb）中任选分离或原位制备的N-氰基-N-烷基烷基磺酰胺反应，其中R 1和R 2具有上述含义，得到 式（Ib）的最终产物。

    Process for the preparation of 4,6-disubstituted 2-isocyanatopyrimidines and their use as intermediates for active compound syntheses
    5.
    发明授权
    Process for the preparation of 4,6-disubstituted 2-isocyanatopyrimidines and their use as intermediates for active compound syntheses 失效
    用于制备4,6-二取代的2-异氰酸基嘧啶的方法及其作为活性化合物合成的中间体的用途

    公开(公告)号：US06365739B1

    公开(公告)日：2002-04-02

    申请号：US09358297

    申请日：1999-07-21

    申请人： Mark James Ford ,  Stephen Lachhein

    发明人： Mark James Ford ,  Stephen Lachhein

    IPC分类号： C07D23942

    CPC分类号： C07D239/545

    摘要： Isocyanates of the formula (I) in which X and Y are defined as in formula (I) of claim 1 can be prepared by reacting a compound of the formula (II) or its salts in which X and Y are defined as in formula (I), with 1 to 6 mol of phosgene per mole of compound of the formula (II), in the presence of 2 to 3.5 molar equivalents of a base per mole of compound of the formula (II) and in the presence of an aprotic organic solvent at a reaction temperature in the range from −30 to +60° C. to give the compound of the formula (I). The compounds (I) can be converted by reaction with nucleophiles to give addition products, such as carbamates, ureas and sulfonylureas and corresponding products, e.g. herbicidal sulfonylureas.

    摘要翻译： 其中X和Y如权利要求1的式（I）中定义的式（I）的异氰酸酯可以通过使式（II）化合物或其盐，其中X和Y如式 ），在每摩尔式（II）化合物的2至3.5摩尔当量的碱存在下，并且在非质子有机物存在下，每摩尔式（II）的化合物具有1至6摩尔的光气 溶剂，反应温度为-30〜+ 60℃，得到式（I）化合物。 化合物（I）可以通过与亲核试剂反应而转化，得到加成产物，例如氨基甲酸酯，脲和磺酰脲类及相应的产品，例如。 除草磺酰脲类。

    [5-CHLORO-6-PHENYL-2-(4-TRIFLUOROMETHYLPHENYL)-4-PYRIMIDINYLAMINO]ACETAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATE OF THESE COMPOUNDS
    7.
    发明授权
    [5-CHLORO-6-PHENYL-2-(4-TRIFLUOROMETHYLPHENYL)-4-PYRIMIDINYLAMINO]ACETAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATE OF THESE COMPOUNDS 失效
    [5-氯代-2-（4-三氟甲基苯基）-4-嘧啶基]氨基]乙酰胺衍生物，其制备方法，含有该化合物的药物组合物和这些化合物的中间体

    公开(公告)号：US06620817B1

    公开(公告)日：2003-09-16

    申请号：US10130151

    申请日：2002-05-13

    申请人： Teruya Murata ,  Kazunori Ohno ,  Masayasu Tanaka ,  Mari Itoh

    发明人： Teruya Murata ,  Kazunori Ohno ,  Masayasu Tanaka ,  Mari Itoh

    IPC分类号： C07D23942

    CPC分类号： C07D239/42

    摘要： A [5-chloro-6-phenyl-2-(4-trifluoromethylphenyl)-4-pyrimidinyl-amino]acetamide derivative of the formula (I): wherein R1 is a methyl group or a cyclopropyl group, and a pharmaceutical composition containing the same. Said compounds exhibit a potent anti-rheumatoid activity and show low toxicity, and hence, they are useful as an agent for prophylaxis or treatment of immuno inflammatory diseases such as rheumatoid diseases (e.g., rheumatoid arthritis, Behcet disease, ankylosing spondylitis, etc.) and autoimmune diseases (e.g., multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, etc.).

    摘要翻译： 式（I）的[5-氯-6-苯基-2-（4-三氟甲基苯基）-4-嘧啶基 - 氨基]乙酰胺衍生物：其中R1是甲基或环丙基，以及含有 相同。 所述化合物显示出有效的抗类风湿活性并显示低毒性，因此它们可用作预防或治疗免疫炎性疾病如类风湿病（例如类风湿性关节炎，白塞病，强直性脊柱炎等） 和自身免疫性疾病（例如，多发性硬化，系统性红斑狼疮，Sjögren综合征等）。

    4,5-disubstituted-2-aminopyrimidines
    8.
    发明授权
    4,5-disubstituted-2-aminopyrimidines 失效
    4,5-二取代-2-氨基嘧啶

    公开(公告)号：US06600037B1

    公开(公告)日：2003-07-29

    申请号：US09692368

    申请日：2000-10-19

    申请人： Jeremy Martin Davis ,  David Festus Charles Moffat

    发明人： Jeremy Martin Davis ,  David Festus Charles Moffat

    IPC分类号： C07D23942

    CPC分类号： C07D239/42 ,  A61K31/505 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12

    摘要： Pyrimidines of formla (1) are described: wherein R1 is a —XR6 group; R2 and R3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, —OH, —OR10 [where R10 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group] —SH, —NO2, —CN, —SR10, —COR10, S(O)R10, —SO2R8, —SO2N(R8)(R9), —CO2R8, —CON(R8)(R9), —CSN(R8)(R9), —NH2 or substituted amino group; R4 is a X1R11 group where X1 is a covalent bond or a —C(R12)(R13)— [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alkyl or haloalkyl group] or —C(O)— group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R5 is a halogen atom or an alkynyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis.

    摘要翻译： 描述了formla（1）的嘧啶：其中R1是-XR6基团; R2和R3可以相同或不同，各自为氢或卤素原子或选自任选取代的脂族，脂环族，杂脂族，杂环脂族， OH，-OR 10 [其中R 10是任选取代的脂族，脂环族，杂脂族，杂脂族，芳族或杂芳族基团] -SH，-NO 2，-CN，-SR 10，-COR 10，S（O）R 10，-SO 2 R 8，-SO 2 N （R8）（R9），-CO2R8，-CON（R8）（R9），-CSN（R8）（R9），-NH2或取代氨基; R4是X1R11基团，其中X1是共价键或-C （R 12）（R 13） - [其中R 12和R 13各自为氢或卤素原子或羟基，烷基或卤代烷基]或-C（O） - 基，R 11为任选取代的苯基，噻吩基，噻唑基或吲哚基 基团; R5是卤素原子或炔基;以及它们的盐，溶剂合物，水合物和N-氧化物。化合物是选择性KDR激酶和/或FGFr激酶抑制剂，并且可用于植物 治疗与血管生成相关的疾病状态。

    Processes for preparing aminophenylsulfonylureas, and intermediates therefor
    9.
    发明授权
    Processes for preparing aminophenylsulfonylureas, and intermediates therefor 有权
    制备氨基苯磺酰脲的方法及其中间体

    公开(公告)号：US06500952B1

    公开(公告)日：2002-12-31

    申请号：US09664201

    申请日：2000-09-18

    申请人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

    发明人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

    IPC分类号： C07D23942

    CPC分类号： C07D521/00 ,  A01N47/36 ,  H01R33/06 ,  Y02A40/143

    摘要： The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A=H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.

    摘要翻译： 本发明涉及化合物（Ⅰ）的制备，其中A = H或酰基，R 1，R 21，R 3，R 4，n，X，Y和Z如权利要求1中所定义，通过卤化和重排化合物 任选的盐），得到化合物（III）a）（III）至（IV）的氨解，硝基的还原和与式Ar-OCO-N（M）-Het的氨基甲酸酯（盐）（VI）的反应， 其中Ar =苯基，M = H或阳离子和Het =来自式（I）的杂环，得到（III）至（IV）化合物（I）（A = H），orb）氨解，与氨基甲酸酯 （VI）和还原所得化合物（VII）在NO 2基团上得到化合物（I）（A = H），orc）（III）与式HNR3-Het的氰酸酯和胺（VIII）的反应，还原 所得到的化合物（Ⅶ）在NO2基团上得到化合物（I）（A = H），任选的酰化如果A不为H.式（I）（A = H），（III） （IV），（V），（VI）（M =阳离子）和（VII）是新颖的。