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1. 发明授权

US4208428A Prostaglandin analogues 失效
标题翻译：前列腺素类似物
公开(公告)号：US4208428A
公开(公告)日：1980-06-17
申请号：US924343
申请日：1978-07-13
申请人： Masayasu Kurono , Nobuyuki Hamanaka , Shigeru Sakuyama , Takeshi Chiba , Hisao Nakai
发明人： Masayasu Kurono , Nobuyuki Hamanaka , Shigeru Sakuyama , Takeshi Chiba , Hisao Nakai
IPC分类号： A61K31/557 , A61K31/19 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12 , C07F9/4018
摘要： The invention relates to prostaglandin analogues of the general formula: ##STR1## (wherein A represents a grouping of the formula: ##STR2## B represents an alkylene group containing from 1 to 7 carbon atoms or a group ##STR3## (wherein the group --(CH.sub.2).sub.n --may be attached to the ortho, meta or para position of the phenyl ring and m and n, which may be the same or different, each represent an integer from 1 to 5 inclusive, the sum of the integers represented by m and n being from 2 to 6 inclusive), X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, W represents ethylene or trans-vinylene, Z represents a halogen atom, and R.sup.1 represents a hydrogen atom or an alkyl group containing from 1 to 12 carbon atoms) and cyclodextrin clathrates of such acids and esters and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, which possess characteristic prostaglandin-like properties.
摘要翻译：本发明涉及以下通式的前列腺素类似物：其中A代表下式的基团：B代表含有1至7个碳原子的亚烷基或基团（IMAGE）（其中基团 - （CH 2）n - 可以连接到苯环的邻位，间位或对位，m和n可以相同或不同，各自表示1至5的整数，包括端值的整数，由 m和n为2至6的整数），X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基，W表示亚乙基或反式亚乙烯基，Z表示卤素原子，R1表示氢原子或烷基含有1至12个碳原子的基团）和这些酸和酯的环糊精包合物，并且当R 1表示氢原子时，其无毒盐具有特征性前列腺素样特性。

2. 发明授权

US4275075A 15-cylobutyl-trans-.DELTA..sup.2 -prostaglandin analogues 失效
标题翻译： 15-cylobutyl-trans-DELTA 2-prostaglandin类似物
公开(公告)号：US4275075A
公开(公告)日：1981-06-23
申请号：US915493
申请日：1978-06-14
申请人： Masayasu Kurono , Hisao Nakai , Shigeru Sakuyama
发明人： Masayasu Kurono , Hisao Nakai , Shigeru Sakuyama
IPC分类号： A61K31/557 , A61K31/19 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07F9/4018
摘要： The present invention relates to prostaglandin analogues of the general formula: ##STR1## [wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents a group of the formula --COOR.sup.4, in which R.sup.4 represents hydrogen or straight- or branched-chain alkyl of 1 to 12 carbon atoms, or a group of the formula --CH.sub.2 OR.sup.5, in which R.sup.5 represents hydrogen or alkylcarbonyl of 2 to 5 carbon atoms and R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent hydrogen, straight- or branched-chain alkyl of 1 to 12 carbon atoms, or an aryl group unsubstituted or substituted by one, two or three substituents selected from alkyl, alkoxy, alkylthio, monoalkylamino and dialkylamino groups and halogen atoms, the alkyl groups or moieties of the said groups containing from 1 to 5 carbon atoms in a straight- or branched-chain, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 is other than hydrogen and the double bond between C.sub.2 -C.sub.3 is trans] and cyclodextrin clathrates of such prostaglandin analogues and, when R.sup.4 in the group - COOR.sup.4 represents hydrogen, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.
摘要翻译：本发明涉及以下通式的前列腺素类似物：其中A表示下式的基团：X表示反式亚乙烯基或亚乙基，Y表示顺式亚乙烯基或亚乙基，R表示式-COOR4，其中R 4表示氢或1至12个碳原子的直链或支链烷基，或式-CH 2 OR 5的基团，其中R 5表示氢或2至5个碳原子的烷基羰基，R 1，R 2 和可以相同或不同的R 3各自表示氢，1至12个碳原子的直链或支链烷基，或未取代或被1,2或3个选自烷基，烷氧基，烷硫基的取代基取代的芳基，单烷基氨基和二烷基氨基和卤素原子，所述基团的直链或支链含有1至5个碳原子的烷基或部分，条件是R1，R2和R3中的至少一个符号是除了氢和 C2-C3之间的双键是反式]和这种前列腺素类似物的环糊精包合物，当组COOR4中的R4表示氢时，其无毒性盐显示出特征性的前列腺素样活性。

3. 发明授权

US4045468A 16-Cyclobutyl-prostaglandins 失效
标题翻译： 16-环丁基 - 前列腺素
公开(公告)号：US4045468A
公开(公告)日：1977-08-30
申请号：US557437
申请日：1975-03-11
申请人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
发明人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07D309/12 , C07F9/4018 , Y10S514/927
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.
摘要翻译：其中A表示下式的组：X表示反式亚乙烯基或亚乙基，Y表示顺式亚乙烯基或亚乙基，R表示氢或1至12个碳原子的烷基，R 1 R 2和R 3表示氢或1〜12个碳原子的烷基或芳基，条件是R1，R2和R3中的至少一个表示烷基或芳基，是具有有用药理特性的新化合物; 它们特别适用于治疗胃溃疡。

4. 发明授权

US4117119A 15-Cyclobutyl-prostaglandins 失效
标题翻译： 15-CYCLOBUTYL-PROSTAGLANDINS
公开(公告)号：US4117119A
公开(公告)日：1978-09-26
申请号：US794580
申请日：1977-05-06
申请人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
发明人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
IPC分类号： C07C51/353 , C07C51/60 , C07C61/04 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00 , C07C51/353 , C07C51/60 , C07C61/04 , C07D309/12 , C07F9/4018 , Y10S514/899 , Y10S514/925
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.

5. 发明授权

US5459049A Motilin-like polypeptide and use thereof 失效
标题翻译：胃动素样多肽及其用途
公开(公告)号：US5459049A
公开(公告)日：1995-10-17
申请号：US3688
申请日：1993-01-13
申请人： Masayasu Kurono , Takahiko Matani , Haruo Takahashi , Kenichi Tanaka , Katsuya Fujimura , Yuji Hayashi , Yohei Kobayashi , Kiichi Sawai
发明人： Masayasu Kurono , Takahiko Matani , Haruo Takahashi , Kenichi Tanaka , Katsuya Fujimura , Yuji Hayashi , Yohei Kobayashi , Kiichi Sawai
IPC分类号： A61K38/00 , C07K14/63 , C12N15/16 , C12N15/63 , C12N15/67
CPC分类号： C07K14/63 , A61K38/00 , C07K2319/02
摘要： A process for the preparation of a polypeptide of the formula ##STR1## wherein A' is Pro, Gly, Asp or Ser; B' is Gly, Asn or Ser; C is Gln, Glu or Asp; D is Asn, Glu or Asp; X' is a residue of amino acid other than Met; E is Gln, Lys or Arg, and Y' is a residue of homoserine or homoserine-lactone, as well as a recombinant DNA and expression plasmid for preparing the polypeptide.
摘要翻译：制备式Phe-Val-A'-Ile-Phe-Thr-Tyr-B'-Glu-Leu-C-TR-Arg-X'-Gln-Glu-Lys-Glu的多肽的方法 -Arg-D-Lys-Gly-EY'，其中A'为Pro，Gly，Asp或Ser; B'是Gly，Asn或Ser; C是Gln，Glu或Asp; D是Asn，Glu或Asp; X'是Met以外的氨基酸残基; E是Gln，Lys或Arg，Y'是高丝氨酸或高丝氨酸 - 内酯的残基，以及用于制备多肽的重组DNA和表达质粒。

6. 发明授权

US5260064A Percutaneous-administration-type pharmaceutical preparation of nitroglycerin 失效
标题翻译：硝酸甘油经皮给药型药物制剂
公开(公告)号：US5260064A
公开(公告)日：1993-11-09
申请号：US680723
申请日：1991-04-04
申请人： Takashi Nakagawa , Hiroko Tsukahara , Masayasu Kurono , Makoto Sato , Tsutomu Ishida , Kazushi Tokita , Mitsuji Nakano
发明人： Takashi Nakagawa , Hiroko Tsukahara , Masayasu Kurono , Makoto Sato , Tsutomu Ishida , Kazushi Tokita , Mitsuji Nakano
IPC分类号： A61K9/70 , A61K31/21 , A61K47/14 , A61L15/58 , A61F13/02
CPC分类号： A61K9/7053 , A61K31/21 , A61K9/7061 , A61L15/58
摘要： A percutaneous-administration-type pharmaceutical preparation of nitroglycerin is provided. The preparation comprises a backing that is impervious to medicines, and a pressure-sensitive adhesive layer that is placed on one surface of said backing, wherein said pressure-sensitive adhesive layer contains an alkyl (meth)acrylate (co)polymer in the concentration of 35-85% by weight, nitroglycerin in the concentration of 10-30% by weight, and a silicic acid anhydride in the concentration of 5-20% by weight, said (co)polymer contains as major (co)polymer components alkyl (meth)acrylates with alkyl groups having 6 or more carbon atoms, which alkyl (meth)acrylates include 2-ethylhexyl methacrylate in the concentration of 40-100% by weight based on the total weight of said alkyl (meth)acrylates. The preparation makes it possible for nitroglycerin to be absorbed percutaneously at a controlled rate for a long period of time. Also, even a compact preparation can supply a sufficient amount of nitroglycerin. Moreover, the preparation can be manufactured at low cost without any complicated process.

7. 发明授权

US5260056A Composition for enhancing biosynthesis of interferon 失效
标题翻译：用于增强干扰素生物合成的组合物
公开(公告)号：US5260056A
公开(公告)日：1993-11-09
申请号：US640750
申请日：1991-01-14
申请人： Kiichi Sawai , Masayasu Kurono , Takahiko Mitani , Naohisa Ninomiya , Yoshiro Ishiwata , Syoji Yokochi , Kyoichi Asano , Kaneo Yamada , Masashi Taki , Takashi Meguro , Mikio Minamitani , Takao Matumoto , Yuichi Shiokawa
发明人： Kiichi Sawai , Masayasu Kurono , Takahiko Mitani , Naohisa Ninomiya , Yoshiro Ishiwata , Syoji Yokochi , Kyoichi Asano , Kaneo Yamada , Masashi Taki , Takashi Meguro , Mikio Minamitani , Takao Matumoto , Yuichi Shiokawa
IPC分类号： A61K31/28 , A61K31/70 , A61K37/66 , A61K31/79 , A61K59/16
CPC分类号： A61K31/28 , A61K31/70
摘要： An organic germanium compound to be effectively used for curing AIDS or making AIDS asymtomatic in various forms is expressed by the following rational formula: ##STR1## wherein n is an integer of 1 or 2 or more, is in the form of a white acicular or needle crystal, shows a solubility of 1.570/100 ml in water at 25.degree. C. and exhibits a melting (decomposition) point of 240.degree. C.
摘要翻译：有效地用于治疗AIDS或以各种形式产生AIDS的有机锗化合物由以下有理式表示：其中n为1或2或更大的整数，为白色针状或针状结晶，在25℃的水中的溶解度为1.570 / 100ml，熔点（分解）为240℃。

8. 发明授权

US5180739A Use of 3-oxygermylpropionic acid to treat and prevent diabetes-dependent type of autoimmune diseases 失效
标题翻译：使用3-甲氧基丙酸治疗并预防糖尿病依赖型自身免疫性疾病
公开(公告)号：US5180739A
公开(公告)日：1993-01-19
申请号：US659649
申请日：1991-02-23
申请人： Kiichi Sawai , Masayasu Kurono , Takahiko Mitani , Masanori Nagabuchi , Keizo Anzai
发明人： Kiichi Sawai , Masayasu Kurono , Takahiko Mitani , Masanori Nagabuchi , Keizo Anzai
IPC分类号： A61K31/28 , A61K31/80 , A61P3/08 , A61P3/10 , A61P37/00
CPC分类号： A61K31/28 , A61K31/80
摘要： A pharmaceutical composition is used to treat and prevent a diabetes-dependent type of autoimmune diseases, said pharmaceutical composition comprising a therapeutically effective amount of 3-oxygermylpropionic acid represented by the following formula:[(O.sub.1/2).sub.3 GeCH.sub.2 CH.sub.2 CO.sub.2 H].sub.nwherein n stands for an integer of 1 or more, optionally with an activating carrier.

9. 发明授权

US5037981A Intermediates for synthesizing BH.sub.4 and its derivatives 失效
标题翻译：用于合成BH4及其衍生物的中间体
公开(公告)号：US5037981A
公开(公告)日：1991-08-06
申请号：US515962
申请日：1990-04-27
申请人： Masayasu Kurono , Takehiko Suzuki , Tomio Ogasawara , Nobuko Ohishi , Kunio Yagi
发明人： Masayasu Kurono , Takehiko Suzuki , Tomio Ogasawara , Nobuko Ohishi , Kunio Yagi
IPC分类号： C07D405/12 , C07D475/04 , C12P25/00
CPC分类号： C07D405/12 , C07D475/04 , C12P25/00
摘要： The present invention relates to intermediates for synthesizing BH.sub.4 and derivatives thereof. The intermediates are shown as follows; ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl, aralkyl, or aryl group; R.sub.2 is an alkyl, hydroxyalkyl, or polyhydroxyalkyl group; R.sub.3 and R.sub.4 are the same or different and represent alkyl, aralkyl, or aryl group; R.sub.5, R.sub.6, R.sub.7, and R.sub.8 are the same or different and represent a hydrogen atom or acyl group; R.sub.9 is an alkyl, aralkyl, or aryl group; R.sub.10 and R.sub.11 are the same or different and represent a hydrogen atom or acyl group; n is an integer of 5 or less; and HX is an acid. The invention also relates to a process for the preparation of L-biopterin.

10. 发明授权

US4970088A Liquid food for supplying protein 失效
标题翻译：用于提供蛋白质的液体食品
公开(公告)号：US4970088A
公开(公告)日：1990-11-13
申请号：US427276
申请日：1989-10-24
申请人： Yoshinaru Tanaka , Sadaaki Iwamura , Naoko Sugiura , Hiromoto Asai , Tadashi Kurachi , Masayasu Kurono , Bunichiro Yasui , Kiichi Sawai
发明人： Yoshinaru Tanaka , Sadaaki Iwamura , Naoko Sugiura , Hiromoto Asai , Tadashi Kurachi , Masayasu Kurono , Bunichiro Yasui , Kiichi Sawai
IPC分类号： A23J3/00 , A23J3/08 , A23L1/09 , A23L1/305
CPC分类号： A23J3/08 , A23L29/30 , A23L33/19 , Y10S426/80 , Y10S426/801
摘要： The invention is a liquid food for supplying protein principally containing protein, seasonings, flavoring materials and water, wherein it contains 5 to 15% by weight of lactalbumin as the protein. The lactalbumin is obtained by heating to denature under conditions so as to form a cloudy solution. The food is useful for undernourished patients who suffer from hypoproteinemia, hypoalbuminemia or common healthy men who need protein so as to desire to supply nutritious food and develop their muscles.

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