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    Leukotriene A4 hydrolase inhibitors
    2.
    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。

    Thiazolidine derivatives
    3.
    发明授权
    Thiazolidine derivatives 失效
    噻唑烷衍生物

    公开(公告)号：US06410576B1

    公开(公告)日：2002-06-25

    申请号：US09744710

    申请日：2001-01-29

    申请人： Kazuo Nishimura ,  Ken-ichi Fujimura ,  Junzo Matsumoto ,  Tadayuki Kobayashi

    发明人： Kazuo Nishimura ,  Ken-ichi Fujimura ,  Junzo Matsumoto ,  Tadayuki Kobayashi

    IPC分类号： A61K31425

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07D277/06 ,  C07K5/0202 ,  C07K5/06052 ,  C07K5/06069 ,  C07K5/06113 ,  C07K5/06139 ,  C07K5/06147 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0819 ,  C07K5/0821

    摘要： An object of the present invention is to provide novel thiazolidine derivatives which are useful as drugs. The thiazolidine derivatives according to the present invention are compounds represented by the following general formula [I] and salts thereof, wherein R1 is alkyl, hydroxy, alkoxy, alkoxyalkyl, phenyl, phenylalkyl, phenylalkoxy, phenoxy, phenoxyalkyl, amino, alkylamino or a nonaromatic heterocycle; R2 is H or alkyl; R3 is H, alkyl or phenyl; R4 is H or alkyl; R5 is alkyl, halogenoalkyl, hydroxy, alkoxy, phenyl, phenylalkoxy, phenoxy, carboxyl, alkoxycarbonyl, phenylalkoxycarbonyl or an aromatic heterocycle; A1 is alkylene; and A2 is alkylene.

    摘要翻译： 本发明的目的是提供可用作药物的新型噻唑烷衍生物。 根据本发明的噻唑烷衍生物是由以下通式[I]表示的化合物及其盐，其中R 1是烷基，羟基，烷氧基，烷氧基烷基，苯基，苯基烷基，苯基烷氧基，苯氧基，苯氧基烷基，氨基，烷基氨基或非芳族 杂环 R2是H或烷基; R3是H，烷基或苯基; R4是H或烷基; 苯基，苯氧基，苯氧基，羧基，烷氧基羰基，苯基烷氧基羰基或芳香族杂环; R 5为烷基，卤代烷基，羟基， A1是亚烷基; 而A2是亚烷基。

    1,3-dialkylurea derivative
    4.
    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

    κ opioid receptor agonist comprising 2-phenylbenzothiazoline derivative
    7.
    发明授权
    κ opioid receptor agonist comprising 2-phenylbenzothiazoline derivative 有权
    κ阿片受体激动剂，其包含2-苯基苯并噻唑啉衍生物

    公开(公告)号：US07112598B2

    公开(公告)日：2006-09-26

    申请号：US10509549

    申请日：2003-03-28

    申请人： Maki Tokai ,  Takahiro Honda ,  Masashi Niwa ,  Yaeko Osumi ,  Ken-ichi Fujimura ,  Shin-ichi Kohno

    发明人： Maki Tokai ,  Takahiro Honda ,  Masashi Niwa ,  Yaeko Osumi ,  Ken-ichi Fujimura ,  Shin-ichi Kohno

    IPC分类号： C07D277/66 ,  C07D417/12 ,  A61K31/428 ,  A61P29/00 ,  A61P25/04

    CPC分类号： C07D417/12 ,  A61K31/428 ,  C07D277/66

    摘要： A compound or a salt thereof having the following formula wherein R1 is acyl, R2 is hydrogen, halogen, unsubstituted alkyl or alkyl substituted by halogen; R3 is halogen or alkoxy; R4 is cycloalkyl, unsubstituted alkyl or alkyl substituted by cycloalkyl, aryl or hydroxyl or an ester thereof or alkoxy; R5 is hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; or R4 and R5 are bonded with each other to form a pyrrolidine ring substituted by hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; R6 is hydroxyl or an ester thereof, alkoxy, alkoxyalkoxy, alkoxyalkoxyalkoxy, mercapto or alkylthio; and A1 and A2, are the same or different, and are alkylene, provided that (i) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by hydroxyl or an ester thereof, R2 is halogen; (ii) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by alkoxyalkyl, R2 is hydrogen; (iii) when R6 is hydroxyl or an ester thereof, R4 is isopropyl.

    摘要翻译： 具有下式的化合物或其盐，其中R 1是酰基，R 2是氢，卤素，未取代的烷基或被卤素取代的烷基; R 3是卤素或烷氧基; R 4是环烷基，未取代的烷基或被环烷基，芳基或羟基或其酯或烷氧基取代的烷基; R 5是羟基或其酯，烷氧基或烷氧基烷基; 或R 4和R 5彼此键合以形成被羟基或其酯取代的吡咯烷环，烷氧基或烷氧基烷基; R 6是羟基或其酯，烷氧基，烷氧基烷氧基，烷氧基烷氧基烷氧基，巯基或烷硫基; 和A 1和A 2各自相同或不同，并且是亚烷基，条件是（i）当R 4和R 0 > 5个彼此键合以形成被羟基或其酯取代的吡咯烷环，R 2是卤素; （ii）当R 4和R 5彼此键合以形成被烷氧基烷基取代的吡咯烷环时，R 2是氢; （iii）当R 6为羟基或其酯时，R 4为异丙基。

    Kappa-opioid receptor agonist comprising 2-phenylbenzothiazoline derivative
    8.
    发明申请
    Kappa-opioid receptor agonist comprising 2-phenylbenzothiazoline derivative 有权
    卡帕阿片受体激动剂包含2-苯基苯并噻唑啉衍生物

    公开(公告)号：US20050113430A1

    公开(公告)日：2005-05-26

    申请号：US10509549

    申请日：2003-03-28

    申请人： Maki Tokai ,  Takahiro Honda ,  Yaeko Osumi ,  Ken-ichi Fujimura

    发明人： Maki Tokai ,  Takahiro Honda ,  Yaeko Osumi ,  Ken-ichi Fujimura

    IPC分类号： A61K31/428 ,  A61P19/02 ,  A61P19/06 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D277/66 ,  C07D417/12

    CPC分类号： C07D417/12 ,  A61K31/428 ,  C07D277/66

    摘要： The present invention provides κ opioid receptor agonists comprising 2-phenylbenzothiazoline derivatives. The present invention relates to κ opioid receptor agonists comprising compounds or salts thereof having the chemical structure represented by the general formula [I]. Namely, it is important for exhibition of the κ opioid receptor agonist actions to have an alkyl group having an amino group at a phenyl group of 2-phenylbenzothiazoline as a substituent and to have an acyl group at a nitrogen atom of 2-phenylbenzothiazoline, wherein R is alkyl having the amino group as the substituent; and R1 is acyl.

    摘要翻译： 本发明提供包含2-苯基苯并噻唑啉衍生物的κ阿片受体激动剂。 本发明涉及具有由通式[I]表示的化学结构的化合物或其盐的κ阿片受体激动剂。 即，对于具有2-苯基苯并噻唑啉的苯基具有氨基的烷基作为取代基并且在2-苯基苯并噻唑啉的氮原子上具有酰基，对于κ阿片受体激动剂作用的展示是重要的，其中 R是具有氨基作为取代基的烷基; R 1是酰基。

    1,3-dialkylurea derivatives having a hydroxyl group
    10.
    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。