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1. 发明授权

US5091403A Sulfinyl imidazole derivatives and antiulcer agents containing the same 失效
标题翻译：磺酰胺咪唑衍生物和含有其的抗体药剂
公开(公告)号：US5091403A
公开(公告)日：1992-02-25
申请号：US565975
申请日：1990-08-10
申请人： Susumu Okabe , Mitsuo Masaki , Tomio Yamakawa , Hitoshi Matsukura , Yutaka Nomura
发明人： Susumu Okabe , Mitsuo Masaki , Tomio Yamakawa , Hitoshi Matsukura , Yutaka Nomura
IPC分类号： F16J15/32 , A61K31/415 , A61K31/4164 , A61P1/04 , A61P35/00 , C07D233/84 , F16C33/78
CPC分类号： C07D233/84
摘要： Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 is hydrogen or an alkyl group having 1-6 carbon atoms, R.sup.2 is an alkyl group having 2-6 carbon atoms substituted with an alkoxy group having 1-4 carbon atoms, each of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently is hydrogen, a halogen, an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, a fluorine-substituted alkyl group having 1-6 carbon atoms, or a fluorine-substituted alkoxy group having 1-6 carbon atoms. The new imidazole derivatives are effective particularly as anti-ulcer agents.

2. 发明授权

US5180836A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US5180836A
公开(公告)日：1993-01-19
申请号：US786392
申请日：1991-11-01
申请人： Susumu Okabe , Mitsuo Masaki , Tomio Yamakawa , Hitoshi Matsukura , Yutaka Nomura
发明人： Susumu Okabe , Mitsuo Masaki , Tomio Yamakawa , Hitoshi Matsukura , Yutaka Nomura
IPC分类号： C07D233/84 , C07D235/28
CPC分类号： C07D233/84 , C07D235/28
摘要： Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R.sup.1 and R.sup.2 are combined to form a heterocyclic ring; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R.sup.3 is combined with R.sup.2 to form a heterocyclic ring; R.sup.8 and R.sup.9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substituent, or R.sup.8 and R.sup.9 are combined to form an alicyclic ring; R.sup.7 is, where R.sup.8 and R.sup.9 are not combined, H, and, where R.sup.8 and R.sup.9 are combined, H, alkyl which may have a substituent, aryl which may have a substituent, arylcarbonyl which may have a substituent, or a sulfur-containing heterocyclic group; and n is 0 or 1. The new imidazole derivatives are effective particularly as anti-ulcer agents.
摘要翻译：公开了具有下式的新的咪唑衍生物：其中R 1和R 2是H，烷基，环烷基，芳基，芳烷基或卤素取代的烷基，或者R 1和R 2结合形成杂环; R3，R4，R5和R6是H，卤素，烷氧基，芳烷氧基，烷基，烷氧基羰基，硝基，氨基，酰基，氟取代的 - 烷基或氟取代的 - 烷氧基，或R3与R2结合形成杂环; R8和R9是可以具有取代基的H，卤素，烷氧基，烷基，烷氧基羰基，硝基，氨基，酰基，氟取代的 - 烷基，氟取代的 - 烷氧基或芳基，或R8和R9组合形成脂环 ; R 7是，其中R 8和R 9不组合，其中R 8和R 9结合，可以具有取代基的烷基，可以具有取代基的芳基，可以具有取代基的芳基或含硫杂环基; 并且n为0或1.新的咪唑衍生物特别用作抗溃疡剂。

3. 发明授权

US5082943A Novel imidazole derivatives 失效
标题翻译：新咪唑衍生物
公开(公告)号：US5082943A
公开(公告)日：1992-01-21
申请号：US658424
申请日：1991-02-20
申请人： Susumu Okabe , Mitsuo Masaki , Tomio Yamakawa , Hitoshi Matsukura , Yutaka Nomura
发明人： Susumu Okabe , Mitsuo Masaki , Tomio Yamakawa , Hitoshi Matsukura , Yutaka Nomura
IPC分类号： A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/47 , A61P1/04 , C07D233/84 , C07D233/86 , C07D233/88 , C07D233/90 , C07D233/92 , C07D235/28 , C07D401/12
CPC分类号： C07D235/28 , C07D233/84
摘要： Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R.sup.1 and R.sup.2 are combined to form a heterocyclic ring; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R.sup.3 is combined with R.sup.2 to form a heterocyclic ring; R.sup.8 and R.sup.9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substituent, or R.sup.8 and R.sup.9 are combined to form an alicyclic ring; R.sup.7 is, where R.sup.8 and R.sup.9 are not combined, H, and, where R.sup.8 and R.sup.9 are combined, H, alkyl which may have a substituent, aryl which may have a substituent, arylcarbonyl which may have a substituent, or a sulfur-containing heterocyclic group; and n is 0 or 1. The new imidazole derivatives are effective particularly as anti-ulcer agents.

4. 发明授权

US5576341A 2-[[2-(N-isobutyl-N-methyl)amino]benzylsulfinyl]-benzimidazole as antimicrobial agent 失效
标题翻译： 2 - [[2-（N-异丁基-N-甲基）氨基]苄基亚磺酰基] - 苯并咪唑作为抗微生物剂
公开(公告)号：US5576341A
公开(公告)日：1996-11-19
申请号：US228750
申请日：1994-04-18
申请人： Mitsuo Masaki , Tomio Yamakawa , Yutaka Nomura , Hitoshi Matsukura
发明人： Mitsuo Masaki , Tomio Yamakawa , Yutaka Nomura , Hitoshi Matsukura
IPC分类号： A01N43/50 , A01N43/52 , A61K31/415
CPC分类号： A61K31/415
摘要： 2-[[2-(N-Isobutyl-N-methyl)amino]benzylsulfinyl]benzimidazole is effective for treating or preventing Helicobacter infections by administration to patients suffering from the infection.
摘要翻译： 2 - [[2-（N-异丁基-N-甲基）氨基]苄基亚磺酰基]苯并咪唑通过给患者感染而治疗或预防幽门螺杆菌感染是有效的。

5. 发明授权

US5070089A Therapeutic agent for liver disease and piperazine derivatives 失效
标题翻译：用于肝病和哌嗪衍生物的治疗剂
公开(公告)号：US5070089A
公开(公告)日：1991-12-03
申请号：US302552
申请日：1989-01-26
申请人： Mitsuo Masaki , Tomio Yamakawa , Masaru Satoh , Hiromitsu Takeda , Yasushi Yoshino , Hitoshi Matsukura
发明人： Mitsuo Masaki , Tomio Yamakawa , Masaru Satoh , Hiromitsu Takeda , Yasushi Yoshino , Hitoshi Matsukura
IPC分类号： C07D295/21 , C07D317/60 , C07H15/26
CPC分类号： C07D295/21 , C07D317/60 , C07H15/26
摘要： A therapeutic agent for liver disease containing as an active ingredient a piperazine derivative having the formula: ##STR1## wherein, A represents a phenyl, p-benzoquinonyl or cumarinyl group which may have at least one substituent selected from the group consisting of halogen, alkyl, fluoroalkyl, formyl, alkoxycarbonyl, acyl, hydroxy, alkoxy, acyloxy, glycosyloxy, amino, alkylamino, mercapto, alkylthio and nitro; B represents a single bond or a straight chain alkylene group containing 1-4 carbon atoms which may have at least one substituent selected from the group consisting of alkyl, aryl, aralkyl, hydroxy and oxo; R represents an atom or a group selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, alkyl, cycloalkyl, aralkyl and aryl; and n is 2 or 3, or its pharmaceutically acceptable salt is disclosed.

6. 发明授权

US5446146A Piperazine derivative having substituted phenyl groups 失效
标题翻译：具有取代苯基的哌嗪衍生物
公开(公告)号：US5446146A
公开(公告)日：1995-08-29
申请号：US255120
申请日：1994-06-07
申请人： Mitsuo Masaki , Tomio Yamakawa , Masaru Satoh , Hiromitsu Takeda , Yasushi Yoshino , Hitoshi Matsukura
发明人： Mitsuo Masaki , Tomio Yamakawa , Masaru Satoh , Hiromitsu Takeda , Yasushi Yoshino , Hitoshi Matsukura
IPC分类号： C07D295/21 , C07D317/60 , C07H15/26 , C07D243/08 , C07D295/194
CPC分类号： C07D295/21 , C07D317/60 , C07H15/26
摘要： A therapeutic agent for liver disease containing as an active ingredient a piperazine derivative having the formula: ##STR1## wherein, A represents a phenyl, p-benzoquinonyl or cumarinyl group which may have at least one substituent selected from the group consisting of halogen, alkyl, fluoroalkyl, formyl, alkoxycarbonyl, acyl, hydroxy, alkoxy, acyloxy, glycosyloxy, amino, alkylamino, mercapto, alkylthio and nitro; B represents a single bond or a straight chain alkylene group containing 1-4 carbon atoms which may have at least one substituent selected from the group consisting of alkyl, aryl, aralkyl, hydroxy and oxo; R represents an atom or a group selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, alkyl, cycloalkyl, aralkyl and aryl; and n is 2 or 8, or its pharmaceutically acceptable salt is diclosed.
摘要翻译：含有下列通式的哌嗪衍生物作为活性成分的肝病治疗剂：其中，A表示可具有至少一个取代基的苯基，对苯醌或类似的基团，所述取代基选自卤素，烷基氟烷基，甲酰基，烷氧基羰基，酰基，羟基，烷氧基，酰氧基，糖氧基，氨基，烷基氨基，巯基，烷硫基和硝基; B表示单键或含有1-4个碳原子的直链亚烷基，其可以具有至少一个选自烷基，芳基，芳烷基，羟基和氧代的取代基; R表示选自氢，碱金属，碱土金属，烷基，环烷基，芳烷基和芳基的原子或基团。并且n为2或8，或其药学上可接受的盐被包围。

7. 发明授权

US5773437A Alkylenediamine derivatives 失效
标题翻译：烷二胺衍生物
公开(公告)号：US5773437A
公开(公告)日：1998-06-30
申请号：US722112
申请日：1996-09-30
申请人： Mitsuo Masaki , Norihisa Miyake , Atsushi Tendo , Michiko Ishida , Haruhiko Shinozaki , Yutaka Nomura , Yasunori Goto
发明人： Mitsuo Masaki , Norihisa Miyake , Atsushi Tendo , Michiko Ishida , Haruhiko Shinozaki , Yutaka Nomura , Yasunori Goto
IPC分类号： C07D275/06 , C07D279/02 , C07D417/06 , A61K31/54
CPC分类号： C07D275/06 , C07D279/02 , C07D279/08 , C07D417/06
摘要： The present invention relates to alkylenediamine derivatives which relieve urinating contraction and therefore are of value as active ingredients of therapeutic agents for treating dysuria.
摘要翻译： PCT No.PCT / JP95 / 00632 Sec。 371日期1996年9月30日 102（e）日期1996年9月30日PCT提交1995年3月31日PCT公布。第WO95 / 26959号公报日期1995年10月12日本发明涉及缓解小便收缩的亚烷基二胺衍生物，因此具有治疗排尿困难的治疗剂的有效成分的价值。

8. 发明授权

US5843992A Epoxysuccinic acid derivatives 失效
标题翻译：环氧琥珀酸衍生物
公开(公告)号：US5843992A
公开(公告)日：1998-12-01
申请号：US930509
申请日：1997-09-29
申请人： Yutaka Nomura , Toshihiro Takahashi , Kaoru Hara , Yasushi Yoshino , Mitsuo Masaki
发明人： Yutaka Nomura , Toshihiro Takahashi , Kaoru Hara , Yasushi Yoshino , Mitsuo Masaki
IPC分类号： C07D303/48 , A61K31/335
CPC分类号： C07D303/48
摘要： An epoxysuccinic acid derivative having the following formula: ##STR1## �wherein R.sup.1 is hydrogen, alkyl, aryl, or aralkyl; each of R.sup.2 and R.sup.3 independently is aryl, aralkyl or alkyl; X is --O-- or --NR.sup.4 --; and R.sup.4 is hydrogen, alkyl, or aralkyl! is useful for prevention and treatment of bone diseases such as osteoporosis, malignant hypercalcemia and Paget's syndrome, and further useful for treatment of osteoarthritis and rheumatoid arthritis which are accompanied by abnormal enhancement of cathepsin L activity, and furthermore useful as a medicine for treating diseases in which cathepsin B and L participate, such as muscular dystrophy and muscular atrophy.
摘要翻译： PCT No.PCT / JP96 / 00889 Sec。 371日期：1997年9月29日 102（e）日期1997年9月29日PCT提交1996年4月1日PCT公布。出版物WO96 / 30354 日期：1996年10月3日具有下式的环氧琥珀酸衍生物：其中R 1是氢，烷基，芳基或芳烷基; R2和R3各自独立地为芳基，芳烷基或烷基; X是-O-或-NR4-; 和R4是氢，烷基或芳烷基]可用于预防和治疗骨质疏松症，恶性高钙血症和佩吉特综合征等骨疾病，并且还可用于治疗组织蛋白酶L活性异常增强的骨关节炎和类风湿性关节炎，并且还可用作治疗组织蛋白酶B和L参与的疾病的药物，例如肌营养不良和肌肉萎缩。

9. 发明授权

US5574030A N-aminoalkyl-substituted nitrogen-containing five membered heterocyclic compounds 失效
标题翻译： N-氨基烷基取代的含氮五元杂环化合物
公开(公告)号：US5574030A
公开(公告)日：1996-11-12
申请号：US91219
申请日：1993-07-13
申请人： Mitsuo Masaki , Norihisa Miyake , Atsushi Tendo , Hiromitsu Takeda , Michiko Ishida , Haruhiko Shinozaki
发明人： Mitsuo Masaki , Norihisa Miyake , Atsushi Tendo , Hiromitsu Takeda , Michiko Ishida , Haruhiko Shinozaki
IPC分类号： C07D263/16 , C07D263/20 , C07D263/22 , C07D263/44 , C07D265/32 , C07D277/14 , C07D413/04 , C07D413/06 , C07D233/32 , A61K31/505 , A61K31/54 , C07D233/42
CPC分类号： C07D263/16 , C07D263/20 , C07D263/22 , C07D263/44 , C07D265/32 , C07D277/14 , C07D413/04 , C07D413/06
摘要： Disclosed are new alkylenediamine derivatives of the following formula which are effective for treatment of dysuria are disclosed: ##STR1## wherein R.sup.1 is hydrogen, alkyl, or a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.2 is a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.3 and R.sup.4 represent hydrogen, alkyl, aralkyl or aryl; or R.sup.3 and R.sup.4 are combined to form one of substituted or unsubstituted 5- to 7-membered heterocyclic groups; X is oxygen, sulfur or imino; Y is oxygen or sulfur; Z is --CH.sub.2 --, --CO-- or --CS--; m is an integer of 0-4; n is an integer of 0-4; r is 0 or 1; and p and q represent an integer of 0-5 provided that p plus q is 1-5.
摘要翻译：公开了对治疗排尿困难有效的下式的新的亚烷基二胺衍生物：其中R 1是氢，烷基或取代或未取代的苯基，萘基或芳族杂环基; R2是取代或未取代的苯基，萘基或芳族杂环基; R3和R4代表氢，烷基，芳烷基或芳基; 或R 3和R 4组合以形成取代或未取代的5至7元杂环基团之一; X是氧，硫或亚氨基; Y是氧或硫; Z是-CH 2 - ， - CO-或-CS-; m为0-4的整数; n是0-4的整数; r为0或1; p和q表示0〜5的整数，只要p + q为1-5。

10. 发明授权

US4804657A Process for protection of brain cells 失效
标题翻译：保护脑细胞的过程
公开(公告)号：US4804657A
公开(公告)日：1989-02-14
申请号：US63379
申请日：1987-06-18
申请人： Kyuya Kogure , Mitsuo Masaki
发明人： Kyuya Kogure , Mitsuo Masaki
IPC分类号： C07D263/20 , A61K31/42 , A61K31/421 , A61K31/445 , A61K31/55 , A61P9/10 , A61P25/28 , A61P43/00 , C07D263/22 , C07D263/24 , A61K31/54
CPC分类号： A61K31/42 , A61K31/445 , A61K31/55
摘要： A process for protection of brain cells which comprises orally or parenterally administering into a man suffering from ischemia or being susceptible to ischemia a 1,3-oxazolidin-2-one derivative having the formula: ##STR1## wherein R is a straight or branched chain alkyl having 3-8 carbon atoms, X is hydrogen, halogen, a lower alkyl or alkoxy, and n is 4, 5 or 6. Representative examples of the active component are (4S,5R)-4-(2-methylpropyl)-5-phenyl-3-(3-piperidinopropyl)-1,3-oxazolidin-2-o ne and (4S,5R)-4-(2-methylpropyl)-3-[3-(perhydroazepin-1-yl)-propyl]-5-phenyl-1,3-oxazolidin-2-one.

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