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    Organic tricyclic compounds
    1.
    发明授权
    Organic tricyclic compounds 失效
    有机三环化合物

    公开(公告)号：US4224344A

    公开(公告)日：1980-09-23

    申请号：US639974

    申请日：1975-12-11

    申请人： Makoto Sunagawa ,  Hiromi Sato ,  Junki Katsube ,  Hisao Yamamoto

    发明人： Makoto Sunagawa ,  Hiromi Sato ,  Junki Katsube ,  Hisao Yamamoto

    IPC分类号： C07C47/235 ,  C07C47/238 ,  C07C47/453 ,  C07C57/50 ,  C07C61/39 ,  C07D295/02 ,  C07D295/03 ,  C07D295/125 ,  C07C87/28 ,  A01N9/24

    CPC分类号： C07D295/03 ,  C07C47/235 ,  C07C47/238 ,  C07C47/453 ,  C07C57/50 ,  C07C61/39 ,  C07D295/125

    摘要： Novel 9-aminoalkyl-methanoanthracenes of the formula: ##STR1## wherein A is C.sub.1 -C.sub.4 alkylene or C.sub.3 -C.sub.4 alkenylene and R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl(C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl or polyhalo(C.sub.2 -C.sub.4)alkyl or, when taken together with the adjacent nitrogen atom, they may form a 5 to 7-membered nitrogen-containing heterocyclic ring which may contain an additional hetero atom, and their non-toxic salts, which are useful as anti-anxiety, anti-depressant, major tranquilizer, anti-histamine and anti-allergy drugs and can be prepared through a novel key intermediate, i.e., 9-formyl-9,10-dihydro-9,10-methanoanthracene, by various methods.

    摘要翻译： 其中A为C 1 -C 4亚烷基或C 3 -C 4亚烯基，R 1和R 2各自为氢，C 1 -C 4烷基，C 3 -C 4烯基，C 3 -C 4炔基，C 3 -C 4炔基， C 1 -C 8环烷基（C 1 -C 3）烷基，芳（C 1 -C 3）烷基或多卤代（C 2 -C 4）烷基，或与相邻的氮原子一起形成5至7元含氮杂环， 可以含有另外的杂原子及其无毒盐，它们可用作抗焦虑剂，抗抑郁剂，主要镇静剂，抗组胺和抗过敏药物，可以通过一种新的关键中间体即9 - 甲酰基-9,10-二氢-9,10-甲烷基蒽。

    9-Formyl-9,10-dihydro-9,10-methanoanthracene
    3.
    发明授权
    9-Formyl-9,10-dihydro-9,10-methanoanthracene 失效
    9-甲酰基-9,10-二氢-9,10-甲烷基蒽

    公开(公告)号：US4358620A

    公开(公告)日：1982-11-09

    申请号：US139740

    申请日：1980-04-14

    申请人： Makoto Sunagawa ,  Hiromi Sato ,  Junki Katsube ,  Hisao Yamamoto

    发明人： Makoto Sunagawa ,  Hiromi Sato ,  Junki Katsube ,  Hisao Yamamoto

    IPC分类号： C07C47/235 ,  C07C47/238 ,  C07C47/453 ,  C07C57/50 ,  C07C61/39 ,  C07D295/02 ,  C07D295/03 ,  C07D295/125 ,  C07C47/52

    CPC分类号： C07D295/03 ,  C07C47/235 ,  C07C47/238 ,  C07C47/453 ,  C07C57/50 ,  C07C61/39 ,  C07D295/125

    摘要： Novel 9-aminoalkyl-methanoanthracenes of the formula: ##STR1## wherein A is C.sub.1 -C.sub.4 alkylene or C.sub.3 -C.sub.4 alkenylene and R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl(C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl or polyhalo(C.sub.2 -C.sub.4)alkyl or, when taken together with the adjacent nitrogen atom, they may form a 5 to 7-membered nitrogen-containing heterocyclic ring which may contain an additional hetero atom, and their non-toxic salts, which are useful as anti-anxiety, anti-depressant, major tranquilizer, anti-histamine and anti-allergy drugs and can be prepared through a novel key intermediate, i.e. 9-formyl-9,10-dihydro-9,10-methanoanthracene, by various methods.

    摘要翻译： 其中A为C 1 -C 4亚烷基或C 3 -C 4亚烯基，R 1和R 2各自为氢，C 1 -C 4烷基，C 3 -C 4烯基，C 3 -C 4炔基，C 3 -C 4炔基， C 1 -C 8环烷基（C 1 -C 3）烷基，芳（C 1 -C 3）烷基或多卤代（C 2 -C 4）烷基，或与相邻的氮原子一起形成5至7元含氮杂环， 可以含有另外的杂原子及其无毒盐，其可用作抗焦虑剂，抗抑郁剂，主要镇静剂，抗组胺和抗过敏药物，并且可以通过新的关键中间体即9- 甲酰基-9,10-二氢-9,10-甲基蒽，通过各种方法。

    Novel morpholine derivatives and the treatment of mental depression
    4.
    发明授权
    Novel morpholine derivatives and the treatment of mental depression 失效
    新型吗啉衍生物和精神抑郁症的治疗

    公开(公告)号：US4085210A

    公开(公告)日：1978-04-18

    申请号：US646908

    申请日：1976-01-06

    申请人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

    IPC分类号： C07D265/30 ,  C07D267/10 ,  C07D409/06 ,  A61K31/535 ,  C07D405/06

    CPC分类号： C07D265/30 ,  C07D267/10

    摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

    摘要翻译： 式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> D-E-代表选自下组的三价基团：CH -CH 2 - 和> C = CH-且C 1和C 2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基，它们的无毒 盐，其可用作抗抑郁药并且可以通过各种方法制备。

    Novel morpholine derivatives and treating depression therewith
    5.
    发明授权
    Novel morpholine derivatives and treating depression therewith 失效
    新型吗啉衍生物和治疗抑郁症

    公开(公告)号：US4169146A

    公开(公告)日：1979-09-25

    申请号：US811944

    申请日：1977-06-30

    申请人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

    IPC分类号： C07D265/30 ,  C07D267/10 ,  A61K27/00

    CPC分类号： C07D265/30 ,  C07D267/10

    摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

    摘要翻译： 式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> DE-表示选自下组的三价基团：CH-CH 2 - 和> C = CH-和C1和C2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基及其无毒盐， 其可用作抗抑郁药并且可以通过各种方法制备。

    Carbapenem compounds
    6.
    发明授权
    Carbapenem compounds 失效
    碳青霉烯化合物

    公开(公告)号：US07115595B2

    公开(公告)日：2006-10-03

    申请号：US10465918

    申请日：2001-12-25

    申请人： Makoto Sunagawa ,  Akira Sasaki

    发明人： Makoto Sunagawa ,  Akira Sasaki

    IPC分类号： C07D477/14 ,  A61K31/407 ,  A61K31/5377 ,  A61K31/496 ,  A61P31/04

    CPC分类号： C07D477/14

    摘要： Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: wherein Ring E is benzene ring or thiophene ring; R1 is optionally OH-substituted C1-3 alkyl; R2 and R3 represent each H, optionally substituted lower alkyl, etc.; R is H, or a group which is hydrolyzed in the living body to regenerate a carboxyl group, etc.; X is O or S; and Y represents H, lower alkyl, etc., or pharmaceutically acceptable salts thereof and medicaments containing said compound as the active ingredient. These compounds exhibit an excellent antibacterial activity over a broad range of Gram-positive and Gram-negative bacteria, in particular, penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae.

    摘要翻译： 具有直接连接到碳青霉烯核的3-位上的取代苯基或取代噻吩的碳青霉烯化合物如下式所示：其中环E是苯环或噻吩环; R 1是任选OH取代的C 1-3烷基; R 2和R 3代表每个H，任选取代的低级烷基等; R是H，或在活体中水解以再生羧基的基团等; X是O或S; 和Y表示H，低级烷基等，或其药学上可接受的盐和含有所述化合物作为活性成分的药物。 这些化合物在广泛的革兰氏阳性和革兰氏阴性细菌，特别是青霉素耐药性肺炎链球菌（PRSP）中表现出优异的抗菌活性，其近年来以高频率分离，因此导致严重的临床问题 和流感嗜血杆菌，由于青霉素结合蛋白（PBP）突变，如β-内酰胺酶非产生氨苄青霉素（BLNAR）流感嗜血杆菌（BLM），其在广泛范围内对现有的β-内酰胺抗生素具有抗药性。

    Bacterial cell wall skeleton component preparaion
    7.
    发明申请
    Bacterial cell wall skeleton component preparaion 审中-公开
    细菌细胞壁骨架成分制备

    公开(公告)号：US20050250175A1

    公开(公告)日：2005-11-10

    申请号：US10522877

    申请日：2003-08-01

    申请人： Takehiko Nomura ,  Makoto Sunagawa ,  Yuko Uenishi

    发明人： Takehiko Nomura ,  Makoto Sunagawa ,  Yuko Uenishi

    IPC分类号： A61K9/00 ,  A61K9/107 ,  A61K9/19 ,  A61K35/74 ,  A61K47/44 ,  A61P37/04 ,  C12Q1/04 ,  C12N1/20

    CPC分类号： C12Q1/04 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/107 ,  A61K9/19 ,  A61K35/74 ,  A61K47/44

    摘要： Novel preparations comprising bacterial cell wall skeleton components and determinations of bacterial cell wall skeleton components are provided. The invention comprises a paste consisting of bacterial cell wall skeleton components (bacteria-CWS) and an oil, and make it possible to provides a paste comprising bacteria-CWS wherein the paste has a viscosity of 0.2 to 0.7 poise (25° C.), an emulsion comprising the same, and a lyophilized formulation. The invention also make it possible to provides evaluation of a pharmaceutical composition comprising bacterial cell wall skeleton components as an effective ingredient, and an intermediate material thereof, assay of their strength, and identification of an effective ingredient by determining the long-chain fatty acid comprised in the bacterial cell wall skeleton components, or a derivative thereof.

    摘要翻译： 提供了包含细菌细胞壁骨架组分和细菌细胞壁骨架组分测定的新型制剂。 本发明包括由细菌细胞壁骨架组分（细菌-CWS）和油组成的糊状物，并且可以提供包含细菌CWS的糊料，其中糊料具有0.2至0.7泊（25℃）的粘度， ，含有它的乳液和冻干制剂。 本发明还可以提供包含细菌细胞壁骨架组分作为有效成分的药物组合物的评价，其中间材料，其强度测定和有效成分的鉴定，通过测定包含的长链脂肪酸 在细菌细胞壁骨架组分中，或其衍生物。

    Novel carbapenem compounds
    8.
    发明申请
    Novel carbapenem compounds 失效
    新型碳青霉烯类化合物

    公开(公告)号：US20050020566A1

    公开(公告)日：2005-01-27

    申请号：US10494603

    申请日：2002-11-01

    申请人： Makoto Sunagawa ,  Akira Sasaki

    发明人： Makoto Sunagawa ,  Akira Sasaki

    IPC分类号： A61P31/04 ,  C07D477/14 ,  A61K31/407 ,  C07D487/04

    CPC分类号： C07D477/14

    摘要： A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.

    摘要翻译： 由下式表示的化合物或其药学上可接受的盐：本发明是一种碳青霉烯化合物，其在宽范围的革兰氏阴性和革兰氏阳性细菌，特别是耐青霉素的肺炎链球菌（PRSP）中具有强的抗菌活性，其已被分离 由于青霉素结合蛋白（PBP）突变如β-内酰胺酶非对称性，近年来出现了严重的临床问题，并且在广泛范围内对现有β-内酰胺类抗生素具有抵抗力的流感嗜血杆菌， 生产氨苄青霉素（BLNAR）流感嗜血杆菌，具有优异的口服吸收能力。

    Process for preparing carbapenem compounds
    10.
    发明授权
    Process for preparing carbapenem compounds 失效
    碳青霉烯化合物的制备方法

    公开(公告)号：US5578722A

    公开(公告)日：1996-11-26

    申请号：US407071

    申请日：1995-03-20

    申请人： Makoto Sunagawa ,  Haruki Matsumura

    发明人： Makoto Sunagawa ,  Haruki Matsumura

    IPC分类号： C07D477/04 ,  C07F9/6561 ,  C07D487/04

    CPC分类号： C07D477/04 ,  C07F9/65611 ,  Y02P20/55

    摘要： Novel and effective process for preparing a carbapenem compound of the formula (III): ##STR1## wherein R.sub.1 and R.sub.2 are each H or lower alkyl, R.sub.3 is lower alkyl, R.sub.4 is a protecting group, L is substituted or unsubstituted arylsulfonyloxy, lower alkanesulfonyloxy, halogeno-lower alkanesulfonyloxy, di-lower alkylphosphoryloxy, etc., and X is H or protected hydroxy, which comprises reacting a .beta.-lactam compound (I) with an acetic acid ester derivative (II), in the presence of base, followed by treating the product with an active esterifying agent for a hydroxy group, said compound (III) being useful as intermediate in preparing 1.beta.-alkylcarbapenem compounds having antibacterial activity.

    摘要翻译： 制备式（III）的碳青霉烯化合物的新颖和有效的方法：其中R1和R2各自为H或低级烷基，R3为低级烷基，R4为保护基，L为取代或未取代的芳基磺酰氧基 ，低级链烷磺酰氧基，卤代低级烷磺酰氧基，二低级烷基磷酰氧基等，X为H或被保护的羟基，其包括使β-内酰胺化合物（I）与乙酸酯衍生物（II）反应， 碱，然后用活性酯化剂处理羟基，所述化合物（III）可用作制备具有抗菌活性的1β-烷基碳青霉烯化合物的中间体。