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    M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity
    5.
    发明申请
    M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity 审中-公开
    具有整合素αvβ3拮抗活性的M取代苯甲酸衍生物

    公开(公告)号：US20050059669A1

    公开(公告)日：2005-03-17

    申请号：US10944712

    申请日：2004-09-21

    申请人： Keiichi Ajito ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Naokazu Yahata ,  Kazuyuki Fujishima ,  Makoto Oyama

    发明人： Keiichi Ajito ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Naokazu Yahata ,  Kazuyuki Fujishima ,  Makoto Oyama

    IPC分类号： C07C229/54 ,  C07C229/60 ,  C07D239/14 ,  C07D239/42 ,  C07D401/12 ,  A61K31/496 ,  A61K31/454 ,  C07D43/02

    CPC分类号： C04B35/632 ,  C07C229/54 ,  C07C229/60 ,  C07D239/14 ,  C07D239/42 ,  C07D401/12

    摘要： An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.

    摘要翻译： 本发明的目的是提供具有整合素α噬菌体拮抗活性的m取代苯甲酸衍生物。 根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物，其可用于治疗或预防心血管疾病，血管生成相关疾病，脑血管疾病，癌症及其转移，免疫疾病 ，骨病和其他疾病：其中A表示任选取代的含有两个氮原子的杂环基团，二等基团等; D表示键，NR 4，CR 5 R 6，O，S或-NR 4 -CR 5 R 6 - 。 X表示CH或N; R 7和R 8代表羟基，烷基等; Q表示> C = O等; R 9表示氢，烷基等; J表示键或亚烷基; R 10表示任选取代的羟基，氨基等; R 11表示氢，烷基等; m为0〜5; n为0〜4; p和q各自为0〜3。

    Perfluoroalkylated aniline compound and process for producing the same
    6.
    发明申请
    Perfluoroalkylated aniline compound and process for producing the same 有权
    全氟烷基化苯胺化合物及其制备方法

    公开(公告)号：US20030204104A1

    公开(公告)日：2003-10-30

    申请号：US10437381

    申请日：2003-05-14

    发明人： Masanobu Onishi ,  Akihiko Yoshiura ,  Eiji Kohno ,  Kenji Tsubata

    IPC分类号： C07C323/29 ,  C07C255/58 ,  C07C229/54

    CPC分类号： C07C323/41 ,  C07C209/68 ,  C07C211/52 ,  C07C213/08 ,  C07C215/76 ,  C07C217/84 ,  C07C233/15 ,  C07C271/14 ,  C07C323/36 ,  C07D209/08

    摘要： The present invention provides an aniline derivative represented by the formula (I) 1 wherein R1 and R2 are each H, (C1-12)alkyl, (C3-8)cycloalkyl, hydroxy(C1-12)alkyl, hydroxycarbonyl (C1-12)alkyl, (C1-6)-alkoxycarbonyl(C1-6)alkyl, nullCOR8, wherein R8 is H, halo-(C1-12)alkyl, (C3-8)cycloalkyl or (substituted) phenyl, COOR9, wherein R9 is a halo(C1-6)alkyl group, (substituted) phenyl or (substituted) benzyl; R3, R4, R5, R6and R7 are each H, halogen, OH, nitro, halo(C1-12)alkylthio, (substituted) amino-(C1-2)alkyl, (substituted) phenyl, (substituted) benzyl, amino, nullN(R10)R11 wherein R10 and R11 are each H, alkyl, cycloalkyl, (substituted) phenyl, (substituted) benzyl, nullCOR8 or COOR9, or (C2-27)perfluoroalkyl, etc., and a process for producing the aniline derivative. According to the process of the present invention, perfluoroalkylaniline derivatives can be obtained by using various anilines as the substrate with a high position selectivity and high yield.

    摘要翻译： 本发明提供由式（I）表示的苯胺衍生物，其中R 1和R 2各自为H，（C 1-12）烷基，（C 3-8）环烷基，羟基（C 1-12）烷基， 羟基羰基（C 1-12）烷基，（C 1-6） - 烷氧基羰基（C 1-6）烷基，-COR 8，其中R 8是H，卤代（C 1-12）烷基，（C 3-8） 环烷基或（取代的）苯基，COOR 9，其中R 9是卤代（C 1-6）烷基，（取代的）苯基或（取代的）苄基; R 3，R 4，R 5，R 6和R 7各自为H，卤素，OH，硝基，卤代（C 1-12）烷硫基，（取代的）氨基 - （C1- 2）烷基，（取代的）苯基，（取代的）苄基，氨基，-N（R 10）R 11，其中R 10和R 11各自为H，烷基，环烷基，（取代的） ，（取代的）苄基，-COR 8或COOR 9或（C2-27）全氟烷基等，以及苯胺衍生物的制备方法。 根据本发明的方法，可以通过以高位置选择性和高收率使用各种苯胺作为基材来获得全氟烷基苯胺衍生物。

    Process for the preparation of esters of aromatic carboxylic acid
    8.
    发明授权
    Process for the preparation of esters of aromatic carboxylic acid 失效
    芳香族羧酸酯的制备方法

    公开(公告)号：US5874608A

    公开(公告)日：1999-02-23

    申请号：US858357

    申请日：1997-05-19

    申请人： Ralf Pfirmann ,  Theodor Papenfuhs

    发明人： Ralf Pfirmann ,  Theodor Papenfuhs

    IPC分类号： C07B61/00 ,  C07C67/11 ,  C07C69/76 ,  C07C227/18 ,  C07C229/54 ,  C07C319/20 ,  C07C323/62

    CPC分类号： C07C67/11

    摘要： The present invention relates to a process for the preparation of compounds of the formula (1)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOR (1)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms or OR, NHR, NR.sub.2, SR or COOR, in which R is an alkyl radical having 1 to 4 carbon atoms, Ar is an aryl radical having 6 to 12 carbon atoms and the radical R shown in formula (1) has the above meaning, by reacting a compound of the formula (2)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOH (2)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms, OH, NH.sub.2, NHR, SH or COOH and Ar has the same meaning as in formula (1), with a sulfate of the formula (RO).sub.2 SO.sub.2, in which R has the above meaning, in the presence of a water-insoluble tertiary amine and water at a temperature of 10.degree. to 120.degree. C. in the presence or absence of a water-insoluble solvent and with the addition of a base, at a pH of 5 to 12.

    摘要翻译： 本发明涉及制备式（1）化合物的方法，R1R2R3R4R5ArCOOR（1）其中R1，R2，R3，R4和R5相同或不同，为氢，卤素，烷基或烷氧基，其具有 1至6个碳原子或OR，NHR，NR 2，SR或COOR，其中R是具有1至4个碳原子的烷基，Ar是具有6至12个碳原子的芳基，并且式（1）中所示的基团R ）具有上述含义，通过使式（2）R 1 R 2 R 3 R 4 R 5 ArCOOH（2）的化合物与其中R 1，R 2，R 3，R 4和R 5相同或不同且为氢，卤素，烷基或烷氧基， 6个碳原子，OH，NH 2，NHR，SH或COOH和Ar的定义与式（1）中的含义相同，式（RO）2 SO 2的硫酸盐，其中R具有上述含义， 水不溶性叔胺和水，在存在或不存在水不溶性溶剂的情况下，在10〜120℃的温度下加入碱，在pH为 5至12。

    Aromatic allylaminonitro compounds, hair dye compositions containing aromatic allylaminonitio compounds, and synthetic and natural fiber dyeing process
    9.
    发明授权
    Aromatic allylaminonitro compounds, hair dye compositions containing aromatic allylaminonitio compounds, and synthetic and natural fiber dyeing process 失效
    芳族烯丙基氨基化合物，含有芳族烯丙基氨基化合物的染发剂组合物，以及合成和天然纤维染色方法

    公开(公告)号：US5685881A

    公开(公告)日：1997-11-11

    申请号：US448448

    申请日：1995-06-30

    申请人： David Rose ,  Horst Hoeffkes ,  Edgar Lieske ,  Iduna Matzik

    发明人： David Rose ,  Horst Hoeffkes ,  Edgar Lieske ,  Iduna Matzik

    IPC分类号： A61K8/00 ,  A61K8/40 ,  A61K8/41 ,  A61Q5/06 ,  A61Q5/10 ,  C07C211/52 ,  C07C215/16 ,  C07C229/54 ,  C09B51/00 ,  D06P1/42 ,  D06P3/04 ,  D06P3/08 ,  D06P3/18 ,  A61K7/13

    CPC分类号： A61K8/418 ,  A61Q5/065 ,  C09B51/00

    摘要： Aromatic allylaminonitro compounds corresponding to formula (I): ##STR1## in which R.sup.1 is hydrogen or an alkyl group containing 1 to 4 carbon atoms, R.sup.2 is hydrogen, an alkyl group containing 1 to 4 carbon atoms or an allyl group CH.sub.2 C(R.sup.5)=CH.sub.2, where R.sup.5 is hydrogen or an alkyl group containing 1 to 4 carbon atoms, R.sup.3 is carboxyl, hydroxy, nitro, halogen or a group NR.sup.6 R.sup.7, where R.sup.6 and R.sup.7 independently of one another represent hydrogen, an alkyl group containing 1 to 4 carbon atoms, a hydroxyalkyl or dihydroxyalkyl group containing 2 to 4 carbon atoms or an allyl group CH.sub.2 C(R.sup.8)=CH.sub.2, where R.sup.8 is hydrogen or an alkyl group containing 1 to 4 carbon atoms, and R.sup.4 is hydrogen or nitro, with the proviso that R.sup.3 and R.sup.4 are not both nitro. The compounds are useful for dyeing fibers, particularly human hair.

    摘要翻译： PCT No.PCT / EP93 / 03303 Sec。 371日期：1995年6月30日 102（e）1995年6月30日PCT 1993年11月25日PCT公布。 公开号WO94 / 12149 日期：1994年6月9日对应于式（I）的芳族烯丙基氨基硝基化合物：其中R 1为氢或含有1至4个碳原子的烷基，R 2为氢，含有1至4个碳原子的烷基 或烯丙基CH 2 C（R 5）= CH 2，其中R 5是氢或含有1至4个碳原子的烷基，R 3是羧基，羟基，硝基，卤素或NR 6 R 7基团，其中R 6和R 7彼此独立地表示氢 ，含有1至4个碳原子的烷基，含2至4个碳原子的羟基烷基或二羟基烷基或烯丙基CH 2 C（R 8）= CH 2，其中R 8是氢或含有1至4个碳原子的烷基，R 4 是氢或硝基，条件是R3和R4不都是硝基。 该化合物可用于染色纤维，特别是人的头发。