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13 条记录 (耗时 0.022 秒)

    Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters
    1.
    发明授权
    Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters 失效
    氨基或胍基-1,2,3,4-四氢-1-萘甲酸酯

    公开(公告)号：US4214093A

    公开(公告)日：1980-07-22

    申请号：US30594

    申请日：1979-04-16

    申请人： Setsuro Fujii ,  Yojiro Sakurai ,  Toyoo Nakayama ,  Ryoji Matsui

    发明人： Setsuro Fujii ,  Yojiro Sakurai ,  Toyoo Nakayama ,  Ryoji Matsui

    IPC分类号： A61K31/00 ,  A61K31/13 ,  A61K31/215 ,  A61K31/24 ,  C07C101/48

    摘要： Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters represented by the formula, ##STR1## wherein R.sub.1 is --NH.sub.2 or ##STR2## R.sub.3 is --H, --R.sub.4, --O--R.sub.4, --NHCOCH.sub.3, a halogen, --CN, ##STR3## --COOH, --COOR.sub.4, ##STR4## or --(CH.sub.2).sub.n --COOCH.sub.2 --CO--R.sub.5 ; R.sub.5 is --O--R.sub.4, --NH.sub.2 or ##STR5## n is 0, 1 or 2, and R.sub.4 is a lower alkyl, or pharmaceutically acceptable acid addition salts thereof. Owing to their inhibitory activity on proteolytic enzymes the said esters and acid addition salts thereof are useful in the therapy of diseases caused by such enzymes.

    摘要翻译： 由下式表示的氨基或胍基-1,2,3,4-四氢-1-萘甲酸酯，其中R 1是-NH 2或者R 3是-H，-R 4， -O-R 4，-NHCOCH 3，卤素，-CN，-COOH，-COOR 4，或者 - （CH 2）n -COOH CH 2 -CO-R 5; R5是-O-R4，-NH2或n是0,1或2，R4是低级烷基或其药学上可接受的酸加成盐。 由于其对蛋白水解酶的抑制活性，所述酯和其酸加成盐可用于治疗由这些酶引起的疾病。

    Amidine compound
    9.
    发明授权
    Amidine compound 失效
    脒化合物

    公开(公告)号：US4454338A

    公开(公告)日：1984-06-12

    申请号：US300534

    申请日：1981-09-09

    申请人： Setsuro Fujii ,  Toshiyuki Okutome ,  Toyoo Nakayama ,  Takashi Yaegashi ,  Masateru Kurumi

    发明人： Setsuro Fujii ,  Toshiyuki Okutome ,  Toyoo Nakayama ,  Takashi Yaegashi ,  Masateru Kurumi

    IPC分类号： C07C249/02 ,  A61K31/155 ,  C07C257/18 ,  C07C279/18 ,  C07D317/68 ,  C07C101/00 ,  C07C101/48

    CPC分类号： C07D317/68 ,  C07C279/18

    摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceuticlly acceptable acid addition salts thereof.

    摘要翻译： 由式＆lt; IMAGE＆gt;表示的脒基化合物及其药学上可接受的酸加成盐是新的化合物，可用作强效的抗胰蛋白胨，抗血浆素，抗激肽释放酶和抗凝血酶剂。 具有强大的抗C1（C1＆upbar＆r，C1＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。 这些脒基化合物通过将式（ⅩⅧ）代表的羧酸化合物与6-脒基-2-萘酚进行常规的酯化反应来制备，如果需要，可以将其转化成其药学上可接受的酸加成盐。

    Amidinonaphthyl furancarboxylate derivatives and acid addition salts therof
    10.
    发明授权
    Amidinonaphthyl furancarboxylate derivatives and acid addition salts therof 失效
    脒基萘基呋喃羧酸酯衍生物和酸加成盐

    公开(公告)号：US5532267A

    公开(公告)日：1996-07-02

    申请号：US215785

    申请日：1994-03-22

    申请人： Toyoo Nakayama ,  Seizo Taira ,  Hiroyuki Kawamura ,  Masaoki Shibuya ,  Masahiro Iwaki

    发明人： Toyoo Nakayama ,  Seizo Taira ,  Hiroyuki Kawamura ,  Masaoki Shibuya ,  Masahiro Iwaki

    IPC分类号： C07D307/68 ,  C07D407/12 ,  A61K31/335 ,  A61K31/34 ,  C07D307/46 ,  C07D317/14

    CPC分类号： C07D407/12 ,  C07D307/68

    摘要： Amidinonaphthyl furancarboxylate derivatives of the formula I ##STR1## wherein A is a single bond or A denotes (a) a phenyl group, cyclopentyl group, or cyclohexyl group,(b) an alkenylphenyl group, alkylphenyl group, phenylalkenyl group, or phenylalkyl group wherein alkyl is C.sub.1 to C.sub.7 alkyl and alkenyl is C.sub.2 to C.sub.7 alkenyl,(c) a C.sub.1 to C.sub.18 alkyl or C.sub.2 to C.sub.7 alkenyl group which may be substituted by one or two substituents selected from C.sub.1 to C.sub.5 alkyl groups and quanidino groups, wherein an alkyl substituent together with the carbon atom to which it is attached may form a cycloalkyl ring having from 3 to 6 carbon atoms, or said C.sub.1 to C.sub.5 alkyl may itself be substituted by a C.sub.3 to C.sub.6 cycloalkyl ring, or(d) --(CH.sub.2).sub.n --NH--CO--(CH.sub.2).sub.n' wherein n and n' may be the same or different and represent an integer from 1 to 4; andwherein R denotes(e) a hydroxyl group,(f) a C.sub.1 to C.sub.7 alkoxy group which may be mono- or disubstituted by C.sub.1 to C.sub.5 alkyl,(g) a phenyl-C.sub.1 -C.sub.4 alkoxy group,(h) --OAl(OH).sub.2,(i) an amino group,(j) ##STR2## or (k) ##STR3## and pharmaceutically acceptable acid addition salts thereof, useful as pharmaceuticals.

    摘要翻译： 其中A是单键或A表示（a）苯基，环戊基或环己基，（b）烯基苯基，烷基苯基，苯基烯基，（C 1 -C 6）烷氧基羰基， 或苯基烷基，其中烷基是C1-C7烷基，烯基是C2-C7链烯基，（c）C1-C18烷基或C2-C7烯基，其可以被一个或两个选自C1-C5烷基和喹啉基的取代基取代 基团，其中烷基取代基与其所连接的碳原子一起可以形成具有3至6个碳原子的环烷基环，或所述C1至C5烷基本身可以被C 3至C 6环烷基环取代，或（d ） - （CH 2）n -NH-CO-（CH 2）n'，其中n和n'可以相同或不同，表示1至4的整数; 并且其中R表示（e）羟基，（f）可被C1至C5烷基单或二取代的C1至C7烷氧基，（g）苯基-C1-C4烷氧基，（h）-OAl（ OH）2，（i）可用作药物的氨基，（j）和/或其药学上可接受的酸加成盐。