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1. 发明授权

US10092589B2 Anti-tumor agent containing anti-tumor platinum complex, and anti-tumor effect enhancer 有权
公开(公告)号：US10092589B2
公开(公告)日：2018-10-09
申请号：US15301807
申请日：2015-04-03
申请人： Taiho Pharmaceutical Company Limited
发明人： Hiroyuki Okabe
IPC分类号： A61K31/555 , A61K31/70 , A61K31/505 , A61K31/7072 , A61K31/513 , A61K33/24
摘要： In order to provide a novel cancer treatment method using a FTD⋅TPI combination drug that exhibits markedly excellent anti-tumor effects with fewer side effects, the present invention provides an anti-tumor agent characterized in that the FTD⋅TPI combination drug and an anti-tumor platinum complex are administered in combination.

2. 发明授权

US5206261A Oxindole derivative 失效
标题翻译： OXINDOLE DERIVATIVE
公开(公告)号：US5206261A
公开(公告)日：1993-04-27
申请号：US663960
申请日：1991-03-20
申请人： Akihiro Kawaguchi , Atsushi Sato , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
发明人： Akihiro Kawaguchi , Atsushi Sato , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
IPC分类号： A61K31/40 , A61K31/44 , C07D209/34 , C07D401/06 , C07D405/06
CPC分类号： C07D401/06 , C07D209/34 , C07D405/06
摘要： The present invention provides an oxindole derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is hydrogen atom, halogen atom, lower alkyl group or lower alkoxyl group, R.sup.2 is hydrogen atom or lower alkyl group, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being alkyl group which may form a ring; benzodioxanyl group; or phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group, diethylamino group, trifluoromethyl group, nitrile group, nitro group and benzyloxy group), R.sup.2 and R.sup.3 may form together .dbd.CH--R.sup.5 (R.sup.5 being same as above), R.sup.4 is 1-propylbutyl group; pyridyl group; or phenyl group which may be substituted by lower alkoxyl group, halogen atom, diethylamino group, benzyloxy group, trifluoromethyl group, nitrile group, nitro group or lower alkyl group.

3. 发明授权

US4529592A Penicillin derivatives 失效
标题翻译：青霉素衍生物
公开(公告)号：US4529592A
公开(公告)日：1985-07-16
申请号：US501560
申请日：1983-06-06
申请人： Ronald G. Micetich , Shigeru Yamabe , Tomio Yamazaki , Naobumi Ishida , Takeshi Ishizawa
发明人： Ronald G. Micetich , Shigeru Yamabe , Tomio Yamazaki , Naobumi Ishida , Takeshi Ishizawa
IPC分类号： C07D499/87 , A61K31/425 , A61K31/43 , A61P31/04 , A61P43/00 , C07D499/00 , C07D499/86 , C07D499/897 , C07F7/10
CPC分类号： C07D499/00 , C07F7/10
摘要： A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 and R.sub.2 are each the same or different and represent hydrogen, C.sub.1-18 alkyl, mononitro-substituted benzyl or group for forming a pharmaceutically acceptable salt and R.sub.3 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkoxymethyl, C.sub.3-8 alkylcarbonyloxymethyl, C.sub.4-9 alkylcarbonyloxyethyl, (C.sub.5-7 cycloalkyl)carbonyloxymethyl, C.sub.9-14 benzylcarbonyloxyalkyl, C.sub.3-8 alkoxycarbonylmethyl, C.sub.4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.-butyrolacton-4-yl, halogenated C.sub.1-6 alkyl substituted with 1 to 3 halogen atoms, C.sub.1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, dimethylaminoethyl, dimethylchlorosilyl, trichlorosilyl, (5-substituted C.sub.1-6 alkyl or phenyl or unsubstituted-2-oxo-1,3-dioxoden-4-yl)methyl, C.sub.8-13 benzoyloxyalkyl and group for forming a pharmaceutically acceptable salt.
摘要翻译：由下式（IMAGE）表示的青霉素衍生物，其中R 1和R 2各自相同或不同，表示氢，C 1-18烷基，一硝基取代的苄基或用于形成药学上可接受的盐的基团，R 3选自氢，C 1-6烷基，C 2-7烷氧基甲基，C 3-8烷基羰基氧基甲基，C 4-9烷基羰基氧基乙基，（C 5-7环烷基）羰基氧基甲基，C 9-14苄基羰氧基烷基，C 3-8烷氧基羰基甲基，C 4-9烷氧基羰基乙基，吡啶-4-基，γ-丁内酯-4-基，被1至3个卤素原子取代的卤代C 1-6烷基，C 1-6烷氧基或硝基取代或未取代的苄基，二苯甲基，四氢吡喃基，二甲基氨基乙基，二甲基氯甲硅烷基，三氯硅烷基（5 取代的C 1-6烷基或苯基或未取代的-2-氧代-1,3-二氧杂环己烯-4-基）甲基，C 13-13苯甲酰氧基烷基和用于形成药学上可接受的盐的基团。

4. 发明授权

US4293713A Novel 1,1,3,5-substituted biuret compound and a pharmaceutical composition containing the same 失效
标题翻译：新颖的1,1,3,5-取代缩二脲化合物和含有它的药物组合物
公开(公告)号：US4293713A
公开(公告)日：1981-10-06
申请号：US134556
申请日：1980-03-27
申请人： Hajime Fujimura , Yasuzo Hiramatsu , Takahiro Yabuuchi , Masakatu Hisaki , Katsuo Takikawa , Takaji Honna , Hidekazu Miyake , Makoto Kajitani
发明人： Hajime Fujimura , Yasuzo Hiramatsu , Takahiro Yabuuchi , Masakatu Hisaki , Katsuo Takikawa , Takaji Honna , Hidekazu Miyake , Makoto Kajitani
IPC分类号： A61K31/17 , A61P25/04 , A61P29/00 , C07C67/00 , C07C239/00 , C07C275/62 , C07C127/24
CPC分类号： C07C275/62 , Y10S514/916
摘要： A novel 1,1,3,5-substituted biuret compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are respectively the same or different, and each are alkyl groups having 1 to 4 carbon atoms; R.sup.3 is a cyclohexyl group or a phenyl group which may be unsubstituted or may have at least one substituent selected from the group consisting of chlorine, bromine, fluorine, methyl, trifluoromethyl, dimethylamino, methoxy, methylthio, nitro and acetyl. The novel 1,1,3,5-substituted biuret compounds are useful as an analgesic, anti-inflammatory and/or anti-pyretic agent.
摘要翻译：下式的新型1,1,3,5-取代缩二脲化合物：其中R 1和R 2分别相同或不同，并且各自为具有1至4个碳原子的烷基; R3是可以是未取代的或可以具有至少一个选自氯，溴，氟，甲基，三氟甲基，二甲基氨基，甲氧基，甲硫基，硝基和乙酰基的取代基的环己基或苯基。新型1,1,3,5-取代的缩二脲化合物可用作止痛剂，抗炎剂和/或抗热解剂。

5. 发明授权

US4287207A Pharmaceutical composition containing 1,3,5-substituted biuret compound 失效
标题翻译：含有1,3,5-取代缩二脲化合物的药物组合物
公开(公告)号：US4287207A
公开(公告)日：1981-09-01
申请号：US134411
申请日：1980-03-27
申请人： Hajime Fujmura , Yasuzo Hiramatsu , Takahiro Yabuuchi , Masakatu Hisaki , Katsuo Takikawa , Takaji Honna , Hidekazu Miyake , Makoto Kajitani
发明人： Hajime Fujmura , Yasuzo Hiramatsu , Takahiro Yabuuchi , Masakatu Hisaki , Katsuo Takikawa , Takaji Honna , Hidekazu Miyake , Makoto Kajitani
IPC分类号： A61K31/17 , C07C273/18 , C07C275/62 , C07D213/40 , C07D213/75 , C07D239/42 , C07D277/48 , C07D317/66 , C07D333/36 , A61K31/145 , A61K31/22 , A61K31/275
CPC分类号： C07D213/40 , A61K31/17 , C07C273/1863 , C07C273/1872 , C07D213/75 , C07D239/42 , C07D277/48 , C07D317/66 , C07D333/36 , Y10S514/825 , Y10S514/916
摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl group having chlorine atom(s), cyano group(s), dimethylamino group(s), hydroxy group(s), methoxy group(s) or carboxy group(s) as the substituent(s), a lower alkenyl group, a hydroxy group, a methoxy group, an acetyl group or a phenyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), methylenedioxy group(s), hydroxy group(s), dimethylamino group(s), carboxy group(s) or carboxymethyl group(s) as the substituent(s), a benzyl group, a pyridyl group, a substituted pyridyl group having methyl group(s) as the substituent(s), a pyridylmethyl group, pyrimidinyl group, a thiazolyl group or a thienyl group, as the active ingredient.
摘要翻译：含有下式的1,3,5-取代缩二脲化合物的镇痛，抗炎或抗裂解组合物，其中R1是氢原子，低级烷基，具有氯原子的取代的低级烷基（s ），氰基，二甲基氨基，羟基，甲氧基或羧基作为取代基，低级烯基，羟基，甲氧基，乙酰基或苯基; R2是氢原子，低级烷基或苯基; R3为苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，亚甲二氧基，羟基，二甲基氨基（二甲基氨基） s），作为取代基的羧基或羧甲基，苄基，吡啶基，具有甲基取代基的取代的吡啶基，吡啶基甲基，嘧啶基，噻唑基或噻吩基作为有效成分。

6. 发明授权

US3935266A N-substituted guanidino acid derivatives 失效
标题翻译： N-取代胍基酸衍生物
公开(公告)号：US3935266A
公开(公告)日：1976-01-27
申请号：US192557
申请日：1971-10-26
申请人： Sadao Hashimoto , Ryuji Sakakibara , Yasushi Kurashige , Katsuo Takikawa , Yoko Osame , Hiroshi Minami , Takashi Suzue
发明人： Sadao Hashimoto , Ryuji Sakakibara , Yasushi Kurashige , Katsuo Takikawa , Yoko Osame , Hiroshi Minami , Takashi Suzue
IPC分类号： A61K31/16 , A61K31/165 , C07C67/00 , C07C239/00 , C07C279/14 , C07C103/30
CPC分类号： C07C279/14
摘要： An N-substituted guanidino acid derivatives having the following formula of ##EQU1## wherein R is an alkyl having 6 to 15 carbon atoms,. a cycloalkyl having 6 to 15 carbon atoms or an aryl(C.sub.6 to C.sub.8)alkyl(C.sub.1 to C.sub.9); A represents R.sup.1 or R.sub.2 CO--, R.sup.1 being an alkyl having 1 to 4 carbon atoms, an alkenyl having 2 to 4 carbon atoms, cyclohexyl, a phenyl containing or not containing a substitute of a lower alkyl, a halogenated lower alkyl, a lower alkoxy, hydroxy or a halogen, or a benzyl containing or not containing a substitute of a lower alkyl, a halogenated lower alkyl, a lower alkoxy, hydroxy or a halogen, and R.sup.2 being an alkyl of 1 to 3 carbon atoms, an alkenyl of 2 to 3 carbon atoms, an aryl of 6 to 8 carbon atoms or an aryl(C.sub.6 to C.sub.8)alkyl(C.sub.1 to C.sub.2); and n is an integer of 4 to 10. The present compounds are excellent in pharmacological activities, particularly in antagonism to bradykinin and histamine, and useful as anti-inflammatory agent.
摘要翻译：具有下式的ANH ANGLE CNH（CH 2）n CONHR NH的N-取代胍基衍生物，其中R是具有6至15个碳原子的烷基。具有6至15个碳原子的环烷基或芳基（C 6至C 8）烷基（C 1至C 9）; A表示R 1或R 2 CO-，R 1为具有1至4个碳原子的烷基，具有2至4个碳原子的烯基，环己基，含有或不含有低级烷基，卤代低级烷基，低级烷氧基，羟基或卤素，或含有或不含低级烷基，卤代低级烷基，低级烷氧基，羟基或卤素的取代基的苄基，R 2为1至3个碳原子的烷基，烯基为2 至3个碳原子，6至8个碳原子的芳基或芳基（C6至C8）烷基（C1至C2）; n为4〜10的整数。本发明化合物的药理活性特别优选缓激肽和组胺的拮抗作用，作为抗炎剂有用。

7. 发明申请

US20020099048A1 Bicycloloactam compounds, use thereof and intermediates for preparing thereof 失效
标题翻译：双环双环内酰胺化合物，其用途及其制备中间体
公开(公告)号：US20020099048A1
公开(公告)日：2002-07-25
申请号：US10041555
申请日：2002-01-10
申请人： Taiho Pharmaceutical Company Limited
发明人： Junji Yamamoto , Takashi Arima , Nobuo Kasahara , Masato Nanri , Kazuo Ogawa , Ichiro Yamawaki , Manabu Kaneda
IPC分类号： A61K031/55 , A61K031/4704 , A61K031/404 , A61K031/4035
CPC分类号： C07D215/227 , A61K31/40 , A61K31/445 , A61K31/47 , A61K31/55 , C07D221/16
摘要： A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects 1 A bicyclolactam derivative represented by the following formula (1) is also disclosed, and is useful as an effective component of an anxiolytic agent 2
摘要翻译：公开了式（1）的双环内酰胺化合物，其具有优异的抗焦虑作用，安全性高，可用作药物的有效成分，其在副作用如催眠，肌肉松弛剂和镇静作用A中大大降低还公开了由下式（1）表示的双环内酰胺衍生物，可用作抗焦虑剂的有效成分

8. 发明授权

US5447944A Carbamoyl-2-pyrrolidinone compounds 失效
标题翻译：氨基甲酰基-2-吡咯烷酮化合物
公开(公告)号：US5447944A
公开(公告)日：1995-09-05
申请号：US216244
申请日：1994-03-22
申请人： Makoto Kajitani , Etsuo Hasegawa , Akihiro Kawaguchi , Junji Yamamoto , Katsuo Toide , Takaji Honna , Mitsugi Yasumoto , Nobuo Kasahara
发明人： Makoto Kajitani , Etsuo Hasegawa , Akihiro Kawaguchi , Junji Yamamoto , Katsuo Toide , Takaji Honna , Mitsugi Yasumoto , Nobuo Kasahara
IPC分类号： C07D207/26 , C07D207/263 , C07D207/273 , C07D401/12 , C07D417/12 , A61K31/425 , A61K31/40 , A61K31/44 , C07D207/12
CPC分类号： C07D207/27 , C07D207/26 , C07D207/273 , C07D401/12 , C07D417/12
摘要： The present invention provides carbamoyl-2 -pyrrolidinone compounds useful as medicaments for improving cerebral functions and activating cerebral metabolism or protecting against anoxic brain damage.
摘要翻译：本发明提供了用作改善脑功能和激活脑代谢或防止缺氧性脑损伤的药物的氨基甲酰基-2-吡咯烷酮化合物。

9. 发明授权

US4814449A Substance 4181-2 失效
标题翻译：物质4181-2
公开(公告)号：US4814449A
公开(公告)日：1989-03-21
申请号：US48297
申请日：1987-05-11
申请人： Qi Chang-qing , Tian Jie , Teruyoshi Marunaka , Yuji Yamada , Ichiro Yamawaki , Toshio Ohtani , Yoshinori Minami , Hitoshi Saito
发明人： Qi Chang-qing , Tian Jie , Teruyoshi Marunaka , Yuji Yamada , Ichiro Yamawaki , Toshio Ohtani , Yoshinori Minami , Hitoshi Saito
IPC分类号： C07D498/14 , C12P17/18 , C07D498/12 , A61K31/33 , A61K31/445
CPC分类号： C07D498/14 , C12P17/188 , C12R1/465 , Y10S514/908
摘要： Disclosed are a compound of the general formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom, an alkyl group or an acyl group, process for the production thereof and use thereof. The compounds have an antitumor activity, and those wherein both of R.sub.1 and R.sub.2 represent a hydrogen atom or an acyl group are novel compounds.
摘要翻译：公开了通式（II）的化合物，其中R 1和R 2相同或不同，各自表示氢原子，烷基或酰基，其制备方法和用途。这些化合物具有抗肿瘤活性，其中R1和R2都表示氢原子或酰基的化合物是新化合物。

10. 发明授权

US4797502A Sulfonic acid ester derivatives and process for preparing same 失效
标题翻译：磺酸酯衍生物及其制备方法
公开(公告)号：US4797502A
公开(公告)日：1989-01-10
申请号：US4610
申请日：1987-01-20
申请人： Setsuro Fujii , Kazuo Ogawa , Toshihiro Hamakawa , Yoshiyuki Muranaka
发明人： Setsuro Fujii , Kazuo Ogawa , Toshihiro Hamakawa , Yoshiyuki Muranaka
IPC分类号： C07C309/73 , C07C143/68
CPC分类号： C07C309/00
摘要： A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the carbon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

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