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22 条记录 (耗时 0.027 秒)

    Urea derivatives and pharmaceutical compositions thereof
    3.
    发明授权
    Urea derivatives and pharmaceutical compositions thereof 失效
    尿素衍生物及其药物组合物

    公开(公告)号：US06492370B1

    公开(公告)日：2002-12-10

    申请号：US09623779

    申请日：2000-09-08

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07C32344

    CPC分类号： C07D295/185 ,  C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D333/32

    摘要： Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S—or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是产生具有尿素结构作为碱性结构并在侧链中具有硫原子和酰胺键的化合物，并找到其药理作用，特别是TNF-α产生抑制作用。本发明提供了由 下式[I]其中R 1是H，烷基，芳族，RA-CO-，RC-S-或式[II]; R2，R3和R4是H，烷基，烯基，环烷基，环烯基或芳族; R5和R6是H，烷基，烯基，环烷基，环烯基或芳族; R5和R6可以一起形成非芳族杂环; R 7是H，烷基，环烷基，羟基，巯基，苯基，RB-O-，RC-S-，RD-COS-，RE-OCO-，RF-N（RG） - 或-CONHOH; 并且A1和A2是亚烷基。

    Leukotriene A4 hydrolase inhibitors
    4.
    发明授权
    Leukotriene A4 hydrolase inhibitors 失效
    白三烯A4水解酶抑制剂

    公开(公告)号：US06242476B1

    公开(公告)日：2001-06-05

    申请号：US09381256

    申请日：1999-09-17

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Ken-ichi Fujimura ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Ken-ichi Fujimura ,  Hiroshi Suhara

    IPC分类号： A61K31401

    CPC分类号： C07D207/16

    摘要： The present invention relates to leukotriene A4 hydrolase inhibitors containing compounds represented by the formula [I] or salts thereof as active ingredients, wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R2 and R3 each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxy, phenylalkoxy, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; “Z” represents sulfur or oxygen; “A” represents alkylene; and “n” represents 0, 1 or 2; providing that the phenyl ring in R1 can be substituted by alkyl, alkoxy or halogen, and that the phenyl ring or the naphthyl ring in R5 can be substituted by alkyl, cycloalkyl, alkoxy, alkylthio or halogen.

    摘要翻译： 本发明涉及含有由式[I]表示的化合物或其盐作为活性成分的白三烯A4水解酶抑制剂，其中R1代表氢，烷基，苯基烷基，烷酰基或苯甲酰基; R2和R3各自表示氢或烷基; R4表示羟基，烷氧基，苯基烷氧基，氨基，烷基氨基或苯基烷基氨基; R5代表苯基烷基或萘基烷基; “Z”表示硫或氧; “A”表示亚烷基; “n”表示0,1或2; 条件是R1中的苯环可以被烷基，烷氧基或卤素取代，R5中的苯环或萘环可以被烷基，环烷基，烷氧基，烷硫基或卤素取代。

    Urea derivatives useful as synthetic intermediates
    6.
    发明授权
    Urea derivatives useful as synthetic intermediates 失效
    尿素衍生物可用作合成中间体

    公开(公告)号：US06730784B2

    公开(公告)日：2004-05-04

    申请号：US10147131

    申请日：2002-05-15

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07D26530

    CPC分类号： C07D295/185 ,  C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D333/32

    摘要： Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S— or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是产生具有尿素结构作为碱性结构并在侧链中具有硫原子和酰胺键的化合物，并找到其药理作用，特别是TNF-α产生抑制作用。本发明提供了由 下式[I]其中R 1是H，烷基，芳基，R A -CO-，R c -S-或式[II]; R 2，R 3和R 4是H，烷基，烯基，环烷基，环烯基或芳族; R 5和R 6是H，烷基，烯基，环烷基，环烯基或芳族; R 5和R 6可以一起形成非芳族杂环; R 7是H，烷基，环烷基，羟基，巯基，苯基，R -O-，R C，-S-，R 6 -COS-，R e -OCO-，R F -N（R G） - 或-CONHOH; A 1和A 2是亚烷基。

    Urea derivatives having nitrogen aromatic heterocycle
    8.
    发明授权
    Urea derivatives having nitrogen aromatic heterocycle 失效
    具有氮芳香杂环的脲衍生物

    公开(公告)号：US06420398B2

    公开(公告)日：2002-07-16

    申请号：US09775420

    申请日：2001-02-01

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07D21302

    CPC分类号： C07D213/40

    摘要： An object of the present invention is to provide novel urea derivatives which have TNF-&agr; production inhibitory effects and are useful as therapeutic agents for various diseases, particularly as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. The urea derivatives according to the present invention are compounds represented by the formula [I] and salts thereof. In the formula, R1 is H, alkyl, phenyl or a group of the formula [`I]; R2 is H, alkyl, carboxyl or ester thereof or the like; R3 and R4 are each H, alkyl, cycloalkyl or the like; R5 is H, alkyl, hydroxy or the like; R6 is a nitrogen aromatic heterocycle; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是提供具有TNF-α产生抑制作用的新型尿素衍生物，可用作各种疾病的治疗剂，特别是作为自身免疫疾病如类风湿性关节炎的治疗剂。 根据本发明的脲衍生物是由式[I]表示的化合物及其盐。 在该式中，R 1是H，烷基，苯基或式[Ⅷ]的基团。 R2是H，烷基，羧基或其酯等; R3和R4各自为H，烷基，环烷基等; R5是H，烷基，羟基等; R6是氮芳香杂环; 并且A1和A2是亚烷基。

    1,3-dialkylurea derivatives having a hydroxyl group
    9.
    发明授权
    1,3-dialkylurea derivatives having a hydroxyl group 失效
    具有羟基的1,3-二烷基脲衍生物

    公开(公告)号：US5891912A

    公开(公告)日：1999-04-06

    申请号：US663239

    申请日：1996-07-15

    申请人： Yoichi Kawashima ,  Ken-ichi Fujimura ,  Hiroshi Suhara ,  Nobuaki Miyawaki ,  Yuko Fujita

    发明人： Yoichi Kawashima ,  Ken-ichi Fujimura ,  Hiroshi Suhara ,  Nobuaki Miyawaki ,  Yuko Fujita

    IPC分类号： C07C275/24 ,  C07D233/64 ,  C07C275/10 ,  A61K31/415

    CPC分类号： C07C275/24 ,  C07C2101/14

    摘要： The present invention related to compounds represented by the following formula (I) and salts thereof, ##STR1## wherein R.sup.1 and R.sup.4 each represents a carboxyl or a carboxyl which is converted into an ester, an amide or hydroxamic acid; R.sup.2 represents a lower alkyl or a phenyl-lower alkyl; R.sup.3 represents a hydrogen atom, a lower alkyl, an amino-lower alkyl, a lower alkylamino-lower alkyl, a hydroxy-lower alkyl, a mercapto-lower alkyl, a carboxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an imidazolyl-lower alkyl, an indolyl-lower alkyl, a (substituted) phenyl group, a (substituted) phenyl-lower alkyl group, a (substituted) naphthyl group, or a (substituted) naphtyl-lower group. The compounds of the present invention have inhibitory effects on endopeptidase 24.11 and are useful as therapeutic agents for cardiovascular disease such as heart failure and hypertension, renal disease such as renal failure, gastroenteric disorder, such as diarrhea and hyperchlorhydria, endocrine and metabolic disease such as obesity, and autoimmune disease such as rheumatism, and as an analgesics for myosalgia and migraine.

    摘要翻译： PCT No.PCT / JP95 / 02236 Sec。 371日期：1996年7月15日 102（e）日期1996年7月15日PCT 1995年11月1日PCT PCT。 WO96 / 14293 PCT出版物 日期：1996年5月17日本发明涉及由下式（I）表示的化合物及其盐，其中R 1和R 4各自表示羧基或被转化为酯的羧基，酰胺或异羟肟基 酸; R2代表低级烷基或苯基 - 低级烷基; R3表示氢原子，低级烷基，氨基 - 低级烷基，低级烷基氨基 - 低级烷基，羟基 - 低级烷基，巯基 - 低级烷基，羧基 - 低级烷基，低级烷氧基羰基 - 低级烷基，咪唑基 - 低级烷基，吲哚基 - 低级烷基，（取代）苯基，（取代的）苯基 - 低级烷基，（取代的）萘基或（取代的）萘基 - 低级基。 本发明的化合物对内肽酶24.11具有抑制作用，可用作心血管疾病如心力衰竭和高血压，肾脏疾病如肾功能衰竭，胃肠疾病如腹泻和高氯酸盐，内分泌和代谢疾病如 肥胖症和自身免疫性疾病如风湿病，以及作为肌营养不良和偏头痛的止痛剂。

    1,3-dialkylurea derivative
    10.
    发明授权
    1,3-dialkylurea derivative 失效
    1,3-二烷基脲衍生物

    公开(公告)号：US5968980A

    公开(公告)日：1999-10-19

    申请号：US849402

    申请日：1997-06-03

    申请人： Yoichi Kawashima ,  Ken-ichi Fujimura ,  Hiroshi Suhara ,  Noriyoshi Yamamoto ,  Hiromi Matsumoto ,  Nobuaki Miyawaki ,  Yuko Fujita

    发明人： Yoichi Kawashima ,  Ken-ichi Fujimura ,  Hiroshi Suhara ,  Noriyoshi Yamamoto ,  Hiromi Matsumoto ,  Nobuaki Miyawaki ,  Yuko Fujita

    IPC分类号： C07C275/24 ,  C07F9/38 ,  C07F9/40 ,  C07C275/18 ,  A61K31/215

    CPC分类号： C07F9/3808 ,  C07C275/24 ,  C07F9/4006 ,  C07C2102/08

    摘要： The present invention relates to compounds represented by the formula [I] and salts thereof, wherein R.sup.1 and R.sup.5 each represents carboxyl, phosphonic or a derivative thereof; R.sup.2 represents hydrogen, lower alkyl, (substituted) phenyl lower alkyl, lower alkoxy or (substituted) phenyl lower alkoxy; R.sup.3 represents lower alkyl or (substituted) phenyl lower alkyl; and R.sup.4 represents a group represented by the formula [XI], [XII] or [XIII]. The compounds of the present invention have endopeptidase 24.11 inhibitory activity and are useful for treating cardiovascular diseases such as heart failure and hypertension, renal diseases such as renal failure, gastroenteric disorders such as diarrhea and hyperchlorhydria, endocrine and metabolic diseases such as obesity, and autoimmune diseases such as rheumatic disease, and for mitigating myosalgia, migraine, etc.

    摘要翻译： PCT No.PCT / JP95 / 02539 Sec。 371日期：1997年6月3日 102（e）日期1997年6月3日PCT 1995年12月19日PCT PCT。 公开号WO96 / 18606 日期：1996年6月20日本发明涉及由式[I]表示的化合物及其盐，其中R1和R5各自表示羧基，膦酸或其衍生物; R 2表示氢，低级烷基，（取代的）苯基低级烷基，低级烷氧基或（取代的）苯基低级烷氧基; R3表示低级烷基或（取代的）苯基低级烷基; 和R 4表示由式[XI]，[XII]或[XIII]表示的基团。 本发明的化合物具有内肽酶24.11抑制活性，可用于治疗心血管疾病如心力衰竭和高血压，肾脏疾病如肾衰竭，肠胃疾病如腹泻和高氯酸盐，内分泌和代谢疾病如肥胖和自身免疫 疾病如风湿病，以及缓解肌肉酸痛，偏头痛等