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1. 发明授权

US06472397B1 Nitrogen-containing heterocyclic compounds having antiplatelet aggregation effect and medicinal use thereof 失效
标题翻译：含有抗血小板聚集作用的含氮杂环化合物及其医药用途
公开(公告)号：US06472397B1
公开(公告)日：2002-10-29
申请号：US09647849
申请日：2000-11-03
申请人： Kazumi Ota , Kazuko Kobayashi , Tomoaki Miura , Takahiro Imai , Kazumasa Aizawa , Hisashi Suzuki , Shokichi Ohuchi , Kiyoaki Katano , Takashi Ando
发明人： Kazumi Ota , Kazuko Kobayashi , Tomoaki Miura , Takahiro Imai , Kazumasa Aizawa , Hisashi Suzuki , Shokichi Ohuchi , Kiyoaki Katano , Takashi Ando
IPC分类号： A61K3144
CPC分类号： C07D401/04 , C07D405/14
摘要： The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.
摘要翻译：公开了式（I）表示的化合物及其药理学上可接受的盐和溶剂合物。该化合物在生物体中水解成由下式表示的化合物，其中W表示氢原子，D表示-V-（CH 2）p -COOR基团，其中R表示氢原子。该化合物通过抑制血小板膜蛋白GPIIb / IIIa与纤维蛋白原的连接来抑制血小板聚集。其中A代表CH 2或CO，B代表基团 - （CH 2）k - 或 - （CH 2）m -CO- X和Y彼此不同，表示N或CH，W表示可在生理条件下除去的酯部分，Z表示基团（II）或（III）：其中D表示基团-V- （CH 2）p -COOR。

2. 发明授权

US07160733B2 Ligand specific to β2-glycoprotein I and use thereof 有权
标题翻译：特异于β2-糖蛋白I的配体及其用途
公开(公告)号：US07160733B2
公开(公告)日：2007-01-09
申请号：US10488688
申请日：2002-01-30
申请人： Eiji Matsuura , Kazuko Kobayashi
发明人： Eiji Matsuura , Kazuko Kobayashi
IPC分类号： G01N33/566 , G01N33/543 , C07J9/00
CPC分类号： G01N33/92 , C07J9/00 , C07J17/00 , G01N33/6893 , Y10S435/975 , Y10S436/815
摘要： The cholesterol derivative, represented by the following formula (1): wherein R represents a C3–C23 saturated or unsaturated aliphatic hydrocarbon residue having an optional substituent, and, to the cholesterol backbone, —OH, —CHO, —COOH, —OOH, or an epoxy group may be added, specifically binds to β2-glycoprotein. By use of the derivative, β2-glycoprotein or a similar substance can be assayed in a very practical manner. Through the assay, a disease can be detected in a very practical manner.
摘要翻译：由下式（1）表示的胆固醇衍生物：其中R表示具有任选取代基的C 3 -C 23饱和或不饱和脂肪族烃残基，对于胆固醇主链，-OH，-CHO，-COOH，-OOH，或可以加入环氧基团，特异性结合β2 - 糖蛋白。通过使用衍生物，可以以非常实用的方式测定β2 - 糖蛋白或类似物质。通过该测定，可以以非常实用的方式检测疾病。

3. 发明授权

US06552057B2 Serotonin 5-HT3 receptor partial activator 失效
标题翻译： 5-羟色胺5-HT3受体部分激活剂
公开(公告)号：US06552057B2
公开(公告)日：2003-04-22
申请号：US09796805
申请日：2001-03-02
申请人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
发明人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
IPC分类号： A61K3142
CPC分类号： C07D263/58 , A61K31/496 , C07D263/30 , C07D413/04
摘要： This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
摘要翻译：本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂，并且不引起便秘作为副作用。特别地，基于以下发现：以下式（2）化合物为代表的新合成苯并恶唑衍生物具有强烈的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体激活作用，本发明提供了这些苯并恶唑衍生物作为5-羟色胺5-HT 3受体部分激活因子。式中，R 1〜R 4可以相同或不同，表示氢原子，卤素原子，取代或未取代的低级烷基，取代或未取代的低级烯基或取代或未取代的氨基，或二 R1和R2的基团可以连接在一起形成环结构，即苯环; R5表示氢原子，取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。

4. 发明授权

US06297246B1 Serotonin 5-HT3, receptor partial activator 失效
标题翻译： 5-羟色胺5-HT3，受体部分活化剂
公开(公告)号：US06297246B1
公开(公告)日：2001-10-02
申请号：US09298952
申请日：1999-04-26
申请人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
发明人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
IPC分类号： A61K31496
CPC分类号： C07D263/58 , A61K31/496 , C07D263/30 , C07D413/04
摘要： This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
摘要翻译：本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂，并且不引起便秘作为副作用。特别地，基于以下结构式（2）所示的新合成的苯并恶唑衍生物具有强的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体活化作用，本发明提供了这些苯并恶唑衍生物作为血清素5-HT3 在上式中，R 1〜R 4可以相同或不同，表示氢原子，卤素原子，取代或未取代的低级烷基，取代或未取代的低级烯基或取代的或未取代的氨基，或两个R 1和R 2可以连接在一起形成环结构，即苯环; R5表示氢原子，取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。

5. 发明授权

US06333328B1 Serotonin 5-HT3 receptor partial activator 失效
标题翻译： 5-羟色胺5-HT3受体部分激活剂
公开(公告)号：US06333328B1
公开(公告)日：2001-12-25
申请号：US09686759
申请日：2000-10-12
申请人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
发明人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
IPC分类号： A61K31495
CPC分类号： C07D263/58 , A61K31/496 , C07D263/30 , C07D413/04
摘要： This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
摘要翻译：本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂，并且不引起便秘作为副作用。特别地，基于以下发现：以下式（2）化合物为代表的新合成苯并恶唑衍生物具有强烈的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体激活作用，本发明提供了这些苯并恶唑衍生物作为5-羟色胺5-HT 3受体部分激活因子。式中，R 1〜R 4可以相同或不同，表示氢原子，卤素原子，取代或未取代的低级烷基，取代或未取代的低级烯基或取代或未取代的氨基，或二 R1和R2的基团可以连接在一起形成环结构，即苯环; R5表示氢原子，取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。

6. 发明授权

US06310056B1 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06310056B1
公开(公告)日：2001-10-30
申请号：US09355272
申请日：1999-07-28
申请人： Yuko Kano , Kazuhiro Aihara , Yumiko Toyooka , Toshiro Sasaki , Hiromasa Takizawa , Kenichi Fushihara , Kazuko Kobayashi , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
发明人： Yuko Kano , Kazuhiro Aihara , Yumiko Toyooka , Toshiro Sasaki , Hiromasa Takizawa , Kenichi Fushihara , Kazuko Kobayashi , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
IPC分类号： A61K31429
CPC分类号： C07D519/00
摘要： The carbapenem derivatives represented by the following formula (I) is disclosed. These compounds have strong anti-bacterial activities against bacteria including methicillin resistant Staphylococcus aureus, penicillin resistant Streptococcus pneumoniae, Enterococci, influenza, and &bgr;-lactamase producing bacteria, and have high stabilities to DHP-1 wherein R1 represents hydrogen or methyl, either one of R2, R3, R4, or R5 represents the bond to the 2-position on the carbapenem ring, and the remaining three respectively represent hydrogen, halogen, nitro, cyano, alkyl, cycloalkyl, alkylthio, alkenyl, formyl, alkylcarbonyl, alkoxycarbonyl, aminosulfonyl, aryl carbonyl, aryl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, lower alkoxyiminomethyl, or hydroxyiminomethyl, R6 is not present or represents alkyl, cycloalkyl, or alkenyl, and R is not present, or represents hydrogen or a group which may be metabolically hydrolyzed in the body, provided that when R6 is not present, R represents hydrogen or a group which may be metabolically hydrolyzed in the body, and when R6 is present, R is not present, and the compound forms an inner salt.
摘要翻译：公开了由下式（I）表示的碳青霉烯衍生物。这些化合物对包括耐甲氧西林金黄色葡萄球菌，青霉素耐药性肺炎链球菌，肠球菌，流感和β-内酰胺酶生产细菌在内的细菌具有很强的抗细菌活性，并且对于DHP-1具有高稳定性，其中R 1表示氢或甲基，R 2 ，R 3，R 4或R 5表示碳青霉烯环上2-位的键，其余3个分别表示氢，卤素，硝基，氰基，烷基，环烷基，烷硫基，烯基，甲酰基，烷基羰基，烷氧基羰基，氨基磺酰基，芳基羰基，芳基，氨基甲酰基，N-低级烷基氨基甲酰基，N，N-二低级烷基氨基羰基，低级烷氧基亚氨基甲基或羟基亚氨基甲基，R6不存在或表示烷基，环烷基或烯基，R不存在，或表示氢或可以在体内代谢水解的基团，条件是当R 6不存在时，R代表氢或可以代谢地水解的基团 e体，当R 6存在时，R不存在，且该化合物形成内盐。

7. 发明授权

US6037342A Serotonin 5-HT.sub.3 receptor partial activator 失效
公开(公告)号：US6037342A
公开(公告)日：2000-03-14
申请号：US852747
申请日：1997-05-06
申请人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
发明人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
IPC分类号： A61K31/42 , A61K31/423 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/5513 , A61P1/00 , A61P1/08 , A61P1/12 , A61P1/14 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P43/00 , C07D263/30 , C07D263/58 , C07D263/60 , C07D413/04 , A61N43/62 , C07D243/08 , C07D403/00
CPC分类号： C07D263/58 , A61K31/496 , C07D263/30 , C07D413/04
摘要： This invention provides a serotonin 5-HT.sub.3 receptor partial activator which has a serotonin 5-HT.sub.3 receptor activating action, in addition to its serotonin 5-HT.sub.3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT.sub.3 receptor antagonism and serotonin 5-HT.sub.3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT.sub.3 receptor partial activators. ##STR1## In the above formula, R.sub.1 to R.sub.4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R.sub.1 and R.sub.2 may be linked together to form a ring structure, namely benzene ring; R.sub.5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.

8. 发明授权

US06867226B2 Serotonin 5-HT3 receptor partial activator 失效
标题翻译： 5-羟色胺5-HT3受体部分激活剂
公开(公告)号：US06867226B2
公开(公告)日：2005-03-15
申请号：US10219496
申请日：2002-08-16
申请人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
发明人： Yasuo Sato , Megumi Yamada , Kazuko Kobayashi , Katsuyoshi Iwamatsu , Fukio Konno , Koichi Shudo
IPC分类号： A61K31/42 , A61K31/423 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/5513 , A61P1/00 , A61P1/08 , A61P1/12 , A61P1/14 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P43/00 , C07D263/30 , C07D263/58 , C07D263/60 , C07D413/04 , A61K31/50
CPC分类号： C07D263/58 , A61K31/496 , C07D263/30 , C07D413/04
摘要： This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect.Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
摘要翻译：本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂，并且不引起便秘作为副作用。特别地，基于以下发现：以下式（2）化合物为代表的新合成苯并恶唑衍生物具有强烈的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体激活作用，本发明提供了这些苯并恶唑衍生物作为5-羟色胺5-HT 3受体部分活化剂。式中，R 1〜R 4可以相同或不同，表示氢原子，卤素原子，取代或未取代的低级烷基，取代或未取代的低级烯基或取代或未取代的氨基，或二 R1和R2的基团可以连接在一起形成环结构，即苯环; R5表示氢原子，取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。

9. 发明授权

US06242437B1 Cephem derivatives 失效
标题翻译： Cephem衍生物
公开(公告)号：US06242437B1
公开(公告)日：2001-06-05
申请号：US09319437
申请日：1999-06-07
申请人： Kazuko Kobayashi , Eijirou Umemura , Kunio Atsumi , Takashi Ida
发明人： Kazuko Kobayashi , Eijirou Umemura , Kunio Atsumi , Takashi Ida
IPC分类号： A61K31546
CPC分类号： C07D519/00
摘要： A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative bacteria including &bgr;-lactamase producing bacteria. In particular, it has higher antimicrobial activity against methicilline-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and imipenem-resistant Pseudomonas aeruginosa than the existing onium salt type cephem derivatives and hence is very useful as a therapeutic agent for infectious diseases derived from various pathogenic bacteria. wherein X represents CH or N, R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or cycloalkyl; any one of R2, R3, R4, and R5 represents R6R7NSO2NH—C1-6 alkyl where R6 and R7, which may be the same or different, represent a hydrogen atom or C1-6 alkyl; and n is 0 or 1.
摘要翻译：公开了由下式（I）表示的化合物。该化合物对革兰氏阳性菌对包括β-内酰胺酶生产细菌在内的Grame-negative细菌的广谱细菌具有有效的抗菌活性。具体而言，与现有的鎓盐型头孢烯衍生物相比，耐甲氧西林金黄色葡萄球菌（MRSA），青霉素耐药性肺炎链球菌（PRSP）和亚胺培南耐药铜绿假单胞菌具有较高的抗菌活性，因此作为治疗剂非常有用用于衍生自各种病原菌的感染性疾病，其中X表示CH或N，R 1表示氢原子，取代或未取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或环烷基; R2，R3，R4和R5中的任一个表示R6R7NSO2NH-C1-6烷基，其中R6和R7可以相同或不同，表示氢原子或C1-6烷基; n为0或1。

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