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1. 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。

2. 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。

3. 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。

4. 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。

5. 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.

6. 发明授权

US5631257A Benzoxazole derivatives 失效
标题翻译：苯并恶唑衍生物
公开(公告)号：US5631257A
公开(公告)日：1997-05-20
申请号：US487697
申请日：1995-06-07
申请人： Katsuyoshi Iwamatsu , Yasuo Sato , Masaaki Izumi , Fukio Konno , Seiji Shibahara , Shigeharu Inoye , Koichi Shudo , Kazuko Amano
发明人： Katsuyoshi Iwamatsu , Yasuo Sato , Masaaki Izumi , Fukio Konno , Seiji Shibahara , Shigeharu Inoye , Koichi Shudo , Kazuko Amano
IPC分类号： A61K31/42 , A61K31/423 , A61K31/495 , A61K31/496 , A61K31/55 , A61P1/00 , A61P1/08 , A61P1/14 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P43/00 , C07D263/58 , C07D263/60 , C07D487/10 , C07D401/00 , C07D419/00
CPC分类号： C07D263/58 , C07D263/60 , C07D487/10
摘要： A benzoxazole derivative of the formula (1) or (2) which has an alicyclic diamine group at the 2-position: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X.sup.-, m and n are defined herein. The compound shows excellent 5-HT.sub.3 receptor antagonism and is useful as an antiemetic agent, a peristalsis controlling agent, an analgesic agent, an antianxiety agent and a schizophrenia treating agent.
摘要翻译：（2）中具有脂环族二胺基团的式（1）或（2）的苯并恶唑衍生物：其中R1，R2，R3，R4，R5，R6， X，m和n在本文中定义。该化合物显示优异的5-HT 3受体拮抗作用，可用作止吐剂，蠕动控制剂，止痛剂，抗焦虑剂和精神分裂症治疗剂。

7. 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。

8. 发明授权

US5661144A Cephem derivatives with 3-substituted bis heterocycles 失效
标题翻译： Cephem衍生物与3-取代的双杂环
公开(公告)号：US5661144A
公开(公告)日：1997-08-26
申请号：US628705
申请日：1996-06-28
申请人： Masaki Tsushima , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura
发明人： Masaki Tsushima , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura
IPC分类号： C07D501/00 , C07D519/06 , A61K31/545 , C07D519/00
CPC分类号： C07D501/00
摘要： Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted 3-(imidazo[5,1-b]thiazolium-6-yl)-1-propenyl as a substituent at the 3-position of the cephem ring: ##STR1##
摘要翻译： PCT No.PCT / JP95 / 01627 Sec。 371日期：1996年6月28日 102（e）日期1996年6月28日PCT提交1995年8月16日PCT公布。出版物WO96 / 05205 日期：2002年2月22日由下式（I）表示的化合物，即具有取代或未取代的3-（咪唑并[5,1-b]噻唑鎓-6-基）-1-丙烯基作为取代基的头孢烯衍生物头脑环的3位：（I）

9. 发明授权

US4151041A Process for production of maltopentaose and maltohexaose 失效
标题翻译：麦芽五糖和麦芽六糖的生产工艺
公开(公告)号：US4151041A
公开(公告)日：1979-04-24
申请号：US826762
申请日：1977-08-22
申请人： Katsuyoshi Iwamatsu , Shoji Omoto , Takashi Shomura , Shigeharu Inoue , Taro Niida , Takashi Hisamatsu , Singo Uchida
发明人： Katsuyoshi Iwamatsu , Shoji Omoto , Takashi Shomura , Shigeharu Inoue , Taro Niida , Takashi Hisamatsu , Singo Uchida
IPC分类号： C12P19/22 , C07H1/06 , C08B37/00 , C12P19/00 , C12P19/04 , C12D13/02 , C12B1/00
CPC分类号： A61K31/70 , C12P19/04 , Y10S435/814 , Y10S435/886
摘要： Maltopentaose and maltohexaose are produced with commercial advantage by cultivation of Streptomyces myxogenes SF-1130 strain under aerobic conditions in an appropriate culture medium and recovery from the resultant culture.
摘要翻译：通过在有氧条件下在合适的培养基中培养粘土链霉菌SF-1130菌株并从所得培养物中回收，产生麦芽五糖和麦芽六糖。

10. 发明授权

US5607927A Cephalosporin derivative 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5607927A
公开(公告)日：1997-03-04
申请号：US385363
申请日：1995-02-07
申请人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/59 , C07D519/00 , C07D519/06 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that contains a thiazolylthio group, an oxazolylthio group or a heterocyclic ring thereof as one of the ring components. The compound according to the present invention has excellent activities to inhibit growth of various bacteria, especially Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), and therefore, the antibacterial agent comprising, as an active ingredient, the inventive compound can be used as a therapeutic drug for the treatment of various bacterial infections. ##STR1##
摘要翻译：作为下述通式（I）表示的氨基噻唑基 - 或氨基噻二唑基 - 头孢菌素衍生物，其具有稠环硫基作为含有噻唑基硫基，恶唑基硫基或其杂环的3位取代基环组件。根据本发明的化合物具有优异的抑制各种细菌，特别是耐甲氧西林金黄色葡萄球菌（MRSA）的革兰氏阳性菌生长的活性，因此作为本发明化合物作为活性成分的抗菌剂可以是用作治疗各种细菌感染的治疗药物。

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