公开(公告)号：EP1437344A1

公开(公告)日：2004-07-14

申请号：EP02768103.0

申请日：2002-09-27

申请人： Takeda Chemical Industries, Ltd.

发明人： MATSUMOTO, Takahiro ,  YAMAMOTO, Masataka ,  NAGABUKURO, Hiroshi ,  MOCHIZUKI, Manabu, Takedayakuhin-suitaryo

IPC分类号： C07C275/38

CPC分类号： C07D207/27 ,  A61K31/17 ,  A61K31/216 ,  A61K31/357 ,  A61K31/36 ,  A61K31/4045 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/55 ,  A61K31/551 ,  C07C275/38 ,  C07C275/42 ,  C07C309/66 ,  C07C311/08 ,  C07C311/21 ,  C07C311/47 ,  C07C317/42 ,  C07C323/42 ,  C07C323/44 ,  C07C323/62 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/14 ,  C07D209/08 ,  C07D209/16 ,  C07D211/46 ,  C07D211/52 ,  C07D211/58 ,  C07D211/62 ,  C07D213/30 ,  C07D213/40 ,  C07D213/56 ,  C07D213/65 ,  C07D213/74 ,  C07D213/75 ,  C07D215/08 ,  C07D215/38 ,  C07D217/02 ,  C07D223/12 ,  C07D233/54 ,  C07D235/30 ,  C07D261/14 ,  C07D277/82 ,  C07D295/13 ,  C07D295/192 ,  C07D295/215 ,  C07D307/14 ,  C07D307/52 ,  C07D317/66 ,  C07D321/10 ,  C07D333/16

摘要： Novel benzene derivatives represented by the formula (I) :
wherein R 1 , R 4 and R 6 each independently represents a hydrogen atom, a halogen atom or a hydrocarbon group, R 2 represents a hydrocarbon group or a heterocyclic group, R 3 represents a hydrocarbon group, NR 7' R 7 or OR 8 (wherein R 7' represents a hydrogen atom or a hydrocarbon group, R 7 represents a non-aromatic group, or R 7' and R 7 may form a ring with the adjacent nitrogen atom, and R 8 represents a hydrocarbon group or a heterocyclic group), R 5 represents a hydrocarbon group or a heterocyclic group (except for a quinolyl group), R 5' represents a hydrogen atom, or a hydrocarbon group, or R 5 and R 5' may form a ring with the adjacent nitrogen atom, and R 5" represents a hydrogen atom or a hydrocarbon group, which have vanilloid receptor agonist activity and are useful as a drug such as an analgesic and an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

摘要翻译： 苯脲衍生物（I）是新的。 式（I）的苯基脲衍生物及其盐和前药是新的。 [图] R1，R4，R6H，卤素或任选取代的烃基; R2烃基或杂环基（均为任选取代的）; R3NR7R7'，OR8或任选取代的烃基; R7'，R5'，R5'H或任选取代的烃基; R7芳族基团; R8烃基或杂环基（均可任意取代）; R5取代的烃基（不含苯甲酰基）或任选取代的杂环基（不包括喹啉基）; 或NR 7 R 7'和/或NR 5 R 5'取代的环。 活动：尿病 止痛; 抗炎; 抗风湿; 抗关节炎; 胃肠道; 抗过敏; 呼吸; 皮肤; 银屑病。 在ICR小鼠的尾部轻弹试验（50℃）中，N- [4-二苯甲氧基-3-丙酰基苯基] -N' - （3,4-二甲氧基苯基）脲（Ia）的ED 50为1mg / 公斤。 作用机制：香草激素。

公开(公告)号：EP1284260A1

公开(公告)日：2003-02-19

申请号：EP01932153.8

申请日：2001-05-21

申请人： Takeda Chemical Industries, Ltd.

发明人： MATSUMOTO, Takahiro ,  KATAYAMA, Nozomi ,  MABUCHI, Hiroshi

IPC分类号： C07D207/333 ,  A61K31/402 ,  A61P43/00 ,  A61P3/10

CPC分类号： C07D207/333 ,  A61K31/402 ,  C07D209/12

摘要： A compound of the formula (I):
   wherein X 1 and X 2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain;
   one of R 1 and R 2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C 1-6 alkoxy group and 2) an optionally substituted carboxy-C 1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and
   R 3 , R 4 and R 5 are the same or different and each is a hydrogen atom or a substituent, or R 4 may link together with R 3 or R 5 to form an optionally substituted ring;
   provided that when R 3 is a hydrogen atom, R 4 is a hydrogen atom and R 5 is methyl, X 2 -R 2 is not 4-cyclohexylphenyl; when R 3 is 4-methoxyphenyl, R 4 is a hydrogen atom and R 5 is methyl, X 2 -R 2 is not 4-methoxyphenyl; and when R 1 or R 2 is a hydrogen atom, the adjacent X 1 or X 2 is not a C 1-7 alkylene;
or a salt thereof exhibits a protein tyrosine phosphatase inhibitory action and is useful as a prophylactic or therapeutic agent for diabetes or the like.

摘要翻译： 式（I）的化合物：其中X1和X2相同或不同，并且各自为主链中的键或具有1至20个原子的间隔基; R 1和R 2之一是具有选自1）任选取代的羧基-C 1-6烷氧基和2）任选取代的羧基-C 1-6脂族烃基的取代基的环状基团，其中所述循环基团任选具有附加 取代基，另一个是任选取代的环状基团或氢原子; 并且R 3，R 4和R 5相同或不同，各自为氢原子或取代基，或者R 4可与R 3或R 5连接形成任选取代的环; 条件是当R3为氢原子时，R4为氢原子，R5为甲基，X2-R2不为4-环己基苯基; 当R3是4-甲氧基苯基时，R4是氢原子，R5是甲基，X2-R2不是4-甲氧基苯基; 当R1或R2为氢原子时，相邻的X1或X2不是C1-7亚烷基; 或其盐表现出蛋白酪氨酸磷酸酶抑制作用，可用作糖尿病等的预防或治疗剂。

公开(公告)号：EP1123928A1

公开(公告)日：2001-08-16

申请号：EP99947961.1

申请日：1999-10-19

申请人： Takeda Chemical Industries, Ltd.

发明人： OI, Satoru ,  SUZUKI, Nobuhiro ,  MATSUMOTO, Takahiro

IPC分类号： C07D243/12 ,  A61K31/551 ,  C07D401/04 ,  C07D403/04 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D243/12

摘要： A compound represented by the formula (I)
[wherein ring B represents a cyclic hydrocarbon group which may have substituent(s); Z represents hydrogen atom or a cyclic group which may have substituent(s); R 1 represents hydrogen atom, a hydrocarbon group which may have substituent(s), a heterocyclic group which may have substituent(s) or an acyl group; R 2 represents amino group which may have substituent(s); D represents a bond or a divalent group; E represents a bond, -CO-, -CON(R a )-, -COO-, -N(R a )CON(R b )-, -N(R a )COO-, -N(R a )SO 2 -, -N(R a )-, -O-, -S-, -SO- or -SO 2 - (R a and R b each independently represents hydrogen atom or a hydrocarbon group which may have substituent(s)); G represents a bond or a divalent group; L represents a bond or a divalent group; A represents hydrogen atom or a substituent; X and Y each represents hydrogen atom or an independent substituent; and ..... represents that R 2 and an atom on ring B may form a ring] or a salt thereof, and a process for producing the same.

摘要翻译： 由式（I）表示的化合物，其中环B表示可具有取代基的环状烃基; Z表示氢原子或可具有取代基的环状基团; R 1表示氢原子，可具有取代基的烃基，可具有取代基的杂环基或酰基; R 2表示可以具有取代基的氨基; D表示键或二价基团; E表示键，-CO-，-CON（R a） - ， - COO - ， - N（R a）CON（R） - ， - N（R a） ，-N（R a）SO 2 - ， - N（R a） - ， - O - ， - S - ， - SO-或-SO 2 - （R a和R b各自独立地表示 氢原子或可具有取代基的烃基）; G表示键或二价基团; L表示键或二价基团; A表示氢原子或取代基; X和Y各自表示氢原子或独立的取代基; 和.....表示R 2和环B上的原子可以形成环或其盐，以及其制备方法。