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1. 发明授权

US5349050A Peptides, and antidementia agents containing the same 失效
标题翻译：肽，和含有它们的抗增生剂
公开(公告)号：US5349050A
公开(公告)日：1994-09-20
申请号：US838140
申请日：1992-02-18
申请人： Mitsuo Masaki , Masaki Uehara , Kenji Hirate , Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima
发明人： Mitsuo Masaki , Masaki Uehara , Kenji Hirate , Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima
IPC分类号： A61K38/00 , C07K5/02 , C07K5/103 , C07K5/117 , C07K7/16 , A61K31/34 , A61K31/02 , C07K5/10 , C07K7/06
CPC分类号： C07K5/0202 , C07K5/1013 , C07K5/1024 , C07K7/16 , A61K38/00
摘要： Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Hat or Cit;if A is D-Pro, B is D-Arg, andif B is D- or L-Arg, A is Sat, Pip, Aze or Arg)Asn-A-L- (D-)Pro-Arg- (Gly)n (A is Set, Thr or Ala, n is 1 or 0)A-Ser-Pip-Arg (A is Pro-Asn-, Asn- or Pro-) ##STR2## (A is cyclopentylcarbonyl, Pro or pGlu; B is Gly or .beta.-Ala, W is a hydrogen atom or a group having the formula:or a peptide having the formula: ##STR3## wherein A and B have the same meanings as mentioned above, respectively pGlu-Asn-Ser-A-B-(Gly)n (A is Aze, D- or L-Pro, Pip or Sat, B is D- or L-Arg, Cit, Hat, Lys or Orn, n is 1 or 0) andPro- (Ash)m-Set-L- (D-)Pro-Arg- (Gly) n (m and n are independently 0 or 1)their functional derivatives, and pharmaceutically acceptable salts thereof.
摘要翻译：公开了具有下式之一的新肽：（A和B是氨基酸：其中如果A是D-或L-Pro，B是Hat或Cit;如果A是D-Pro，B是D -Arg，如果B为D-或L-Arg，A为Sat，Pip，Aze或Arg）Asn-AL-（D-）Pro-Arg-（Gly）n（A为Set，Thr或Ala，n （A为Pro-Asn-，Asn-或Pro-）A（A为环戊基羰基，Pro或pGlu; B为Gly或β-Ala，W为氢原子或具有下式的基团：或具有下式的肽：其中A和B分别具有与上述相同的含义，分别为pGlu-Asn-Ser-AB-（Gly）n（A为Aze，D- 或L-Pro，Pip或Sat，B为D-或L-Arg，Cit，Hat，Lys或Orn，n为1或0）和Pro-（Ash）m-Set-L-（D- Arg-（Gly）n（m和n独立地为0或1）它们的官能衍生物及其药学上可接受的盐。

2. 发明授权

US5112947A Peptides, and antidementia agents containing the same 失效
标题翻译：肽，以及含有它的抗生素代谢物
公开(公告)号：US5112947A
公开(公告)日：1992-05-12
申请号：US509950
申请日：1990-04-16
申请人： Mitsuo Masaki , Masaki Uehara , Kenji Hirate , Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima
发明人： Mitsuo Masaki , Masaki Uehara , Kenji Hirate , Yoshikazu Isowa , Yoshiaki Sato , Yoshiharu Nakashima
IPC分类号： A61K38/00 , C07K5/02 , C07K5/103 , C07K5/117 , C07K7/16
CPC分类号： C07K5/0202 , C07K5/1013 , C07K5/1024 , C07K7/16 , A61K38/00
摘要： Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Har or Cit;if A is D-Pro, B is D-Arg, andif B is D- or L-Arg, A is Sar, Pip, Aze or Arg)Asn-A-L-(D-)Pro-Arg-(Gly).sub.n(A is Ser, Thr or Ala, n is 1 or 0)A-Ser-Pip-Arg(A is Pro-Asn-, Asn- or Pro-) ##STR2## (A is cyclopentylcarbonyl, Pro or pGlu; B is Gly or .beta.-Ala, W is a hydrogen atom or a group having the formula: or a peptide having the formula: ##STR3## wherein A and B have the same meanings as mentioned above, respectivelypGlu-Asn-Ser-A-B-(Gly).sub.n(A is Aze, D- or L-Pro, Pip or Sar, B is D- or L-Arg, Cit, Har, Lys or Orn, n is 1 or 0) andPro-(Asn).sub.m -Ser-L-(D-)Pro-Arg-(Gly).sub.n(m and n are independently 0 or 1)their functional derivatives, and pharmaceutically acceptable salts thereof.

3. 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。

4. 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.

5. 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。

6. 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.

7. 发明授权

US4155932A Method for non-catalytically producing tertiary phosphine dichlorides 失效
标题翻译：非催化生产叔膦二氯化物的方法
公开(公告)号：US4155932A
公开(公告)日：1979-05-22
申请号：US918561
申请日：1978-06-23
申请人： Mitsuo Masaki , Susumu Fuzimura
发明人： Mitsuo Masaki , Susumu Fuzimura
IPC分类号： A61K31/28 , C07F9/535 , C07F9/52
CPC分类号： C01B31/00 , A61K31/28 , C01B31/26 , C01B31/28 , C07F9/535
摘要： Tertiary phosphine dichlorides are non-catalytically produced by directly reacting chlorine and carbon monoxide with a tertiary phosphine oxide preferably in a halogenated hydrocarbon solvent at a temperature of from -20.degree. to 100.degree. C.
摘要翻译：叔膦二氯化物是通过在-20℃至100℃的温度下直接使氯和一氧化碳与叔膦氧化物优选在卤代烃溶剂中直接反应而非催化产生的。

8. 发明授权

US4133831A Process for catalytically producing phosgene 失效
标题翻译：催化生产光气的方法
公开(公告)号：US4133831A
公开(公告)日：1979-01-09
申请号：US885605
申请日：1978-03-13
申请人： Mitsuo Masaki , Susumu Fuzimura
发明人： Mitsuo Masaki , Susumu Fuzimura
IPC分类号： C01B32/80 , A61K31/28 , C07F9/02
CPC分类号： C01B31/00 , A61K31/28 , C01B31/26 , C01B31/28
摘要： Disclosed is a process for catalytically producing phosgene in a high yield in a solvent. In this process, carbon monoxide gas is brought into contact with a solution containing chlorine and with a catalyst consisting of at least one phosphine chloride compound, so as to cause the carbon monoxide to react with the chlorine. The phosphine chloride catalyst compound can be selected from substituted and unsubstituted trialkylphosphine dichlorides, substituted and unsubstituted tetraalkyldiphosphine tetrachlorides, substituted and unsubstituted alkylphosphorane dichlorides, and substituted and unsubstituted alkylene-bis(alkylphosphine) tetrachlorides.
摘要翻译：公开了在溶剂中以高产率催化生产光气的方法。在该过程中，一氧化碳气体与含氯溶液和由至少一种氯化膦化合物组成的催化剂接触，以使一氧化碳与氯反应。氯化膦催化剂化合物可以选自取代和未取代的三烷基二氯化膦，取代和未取代的四烷基二膦四氯化物，取代和未取代的烷基二氯化磷，以及取代和未取代的亚烷基 - 二（烷基膦）四氯化物。

9. 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。

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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