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1. 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。

2. 发明授权

US5852006A N-aminoalkyl-substituted nitrogen-containing six membered heterocyclic compounds 失效
标题翻译： N-氨基烷基取代的含氮六元杂环化合物
公开(公告)号：US5852006A
公开(公告)日：1998-12-22
申请号：US725247
申请日：1996-10-04
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 , C07D413/06 , C07D265/30 , A61K31/535 , A61K31/54 , C07D279/12
CPC分类号： C07D263/16 , C07D263/20 , C07D263/22 , C07D263/44 , C07D265/32 , 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。

3. 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。

4. 发明授权

US5310902A Alkylenediamine derivatives 失效
标题翻译：烷二胺衍生物
公开(公告)号：US5310902A
公开(公告)日：1994-05-10
申请号：US741590
申请日：1991-08-07
申请人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
发明人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
IPC分类号： C07D295/13 , C07D223/00 , C07D211/26
CPC分类号： C07D295/13
摘要： Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.
摘要翻译：新型亚烷基二胺衍生物有效地可用的谷氨酸盐阻滞剂具有式（I）或（II）：其中R 1和R 6各自为脂族烃基，脂环族烃基，芳基，或芳烷基; R 2和R 7各自为脂族烃基，烷氧基，含酯键的脂族烃基，含有醚键的脂族烃基或芳氧基; R 3，R 4，R 5，R 9和R 10各自为氢，烷基，烷氧基，酰氧基，芳基，芳烷基，羟基，羟基烷基，卤素，腈，硝基，氨基，氨基甲酰基或烷氧基羰基; 并且m和n分别为0-3的整数（m + n不超过3）; k是1-4的整数; p和i中的每一个是2-13的整数; 并且q和j中的每一个是4-7的整数。

5. 发明授权

US5250546A Amino-alcohol derivatives and processes for their preparation 失效
标题翻译：氨基醇衍生物及其制备方法
公开(公告)号：US5250546A
公开(公告)日：1993-10-05
申请号：US551037
申请日：1990-07-11
申请人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
发明人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
IPC分类号： C07D295/13 , A61K31/445
CPC分类号： C07D295/13
摘要： Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.
摘要翻译：其中R1是具有3至8个碳原子的直链或支链烷基，R2和R3各自为低级烷基，或R2和R3形成5-至7-元环的下式的氨基醇衍生物，与可能具有氧原子的相邻氮原子一起，R4是氢原子或低级烷基，R5是氢原子或低级烷基，X是氢或卤素原子或低级烷基或低级烷基烷氧基，n为2或3的整数，其酸加成盐可有效用作药物和农药。还公开了制备这些化合物的方法。

6. 发明授权

US4764617A Quinaldinamide derivatives 失效
标题翻译：喹哪啶衍生物
公开(公告)号：US4764617A
公开(公告)日：1988-08-16
申请号：US895938
申请日：1986-08-13
申请人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
发明人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
IPC分类号： C07D295/12 , A01N43/42 , A61K31/47 , A61K31/55 , A61P25/00 , C07C67/00 , C07C209/00 , C07C209/40 , C07C209/60 , C07C211/27 , C07C213/00 , C07C225/16 , C07C239/00 , C07C251/48 , C07D20060101 , C07D215/48 , C07D215/52 , C07D217/00 , C07D295/10 , C07D401/06 , C07D401/12
CPC分类号： C07D215/48 , Y10S514/906
摘要： A novel quinaldinamide derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents a lower alkyl group or R.sup.1 and R.sup.2 are combined together with the adjacent nitrogen atom to form a 5-7 membered ring; and X represents the hydrogen atom, a lower alkyl group or a lower alkoxy group, and its acid-addition salt, which show prominent central muscle relaxant effect, namely rigidity relieving effect on anemic decerebrated rigidity.

7. 发明授权

US5070196A Alkylenediamine derivatives 失效
标题翻译：烷二胺衍生物
公开(公告)号：US5070196A
公开(公告)日：1991-12-03
申请号：US562422
申请日：1990-08-01
申请人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
发明人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
IPC分类号： C07D295/13
CPC分类号： C07D295/13
摘要： Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.
摘要翻译：作为谷氨酸盐阻滞剂有效利用的新型亚烷基二胺衍生物具有式（I）或（II）：其中R 1和R 6各自为脂族烃基，脂环族烃基，芳基基团或芳烷基; R 2和R 7各自为脂族烃基，烷氧基，含酯键的脂族烃基，含有醚键的脂族烃基或芳氧基; R 3，R 4，R 5，R 8，R 9和R 10各自为氢，烷基，烷氧基，酰氧基，芳基，芳烷基，羟基，羟烷基，卤素，腈，硝基，氨基，氨基甲酰基或烷氧基羰基; 并且m和n分别为0-3的整数（m + n不超过3）; k是1-4的整数; p和i中的每一个是2-13的整数; 并且q和j中的每一个是4-7的整数。

8. 发明授权

US5312811A Peptide derivatives and antidemetia agents 失效
标题翻译：肽衍生物和抗细菌剂
公开(公告)号：US5312811A
公开(公告)日：1994-05-17
申请号：US393515
申请日：1989-08-14
申请人： Mitsuo Masaki , Seiji Kondo , Norihisa Miyake , Masaki Uehara , Kenji Hirate , Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima
发明人： Mitsuo Masaki , Seiji Kondo , Norihisa Miyake , Masaki Uehara , Kenji Hirate , Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima
IPC分类号： A61K38/00 , C07K5/10 , C07K5/117 , C07K7/16 , A61K37/02 , C07K7/06
CPC分类号： C07K5/1024 , C07K7/16 , A61K38/00
摘要： A novel peptide derivative having the formula: ##STR1## wherein A between Pro and Q.sup.2 is Arg or Lys: Q.sup.1 is pGlu or H; Q.sup.2 is --Gly--OH or OH; Y.sup.1 is H or --CO--T and Y.sup.2 is OH or T; wherein T is a thiamine derivative group is disclosed. The peptide derivative shows a remarkable nootropic effect.
摘要翻译：具有下式的新型肽衍生物：其中Pro和Q2之间的A是Arg或Lys：Q1是pGlu或H; Q2是-Gly-OH或OH; Y1是H或-CO-T，Y2是OH或T; 其中T是硫胺素衍生物基团。肽衍生物显示出显着的向异性作用。

9. 发明授权

US5180712A Petide antidementia and nootropic agents 失效
标题翻译：皮质类抗生素和非特异性药物
公开(公告)号：US5180712A
公开(公告)日：1993-01-19
申请号：US393572
申请日：1989-08-14
申请人： Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima , Mitsuo Masaki , Norihisa Miyake , Masaki Uehara , Kenji Hirate
发明人： Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima , Mitsuo Masaki , Norihisa Miyake , Masaki Uehara , Kenji Hirate
IPC分类号： A61K38/00 , C07K5/113 , C07K7/16
CPC分类号： C07K5/1021 , C07K7/16 , A61K38/00
摘要： A peptide having one of the following formulae (I), (II), (III) and (IV): ##STR1## or its functional derivatives, and a pharmaceutically acceptable salt thereof are disclosed. These peptides have a nootropic effect and are effective as antidementia agents.

10. 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.

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