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1. 发明授权

US5763673A Diarylheptanoide derivative and pharmaceutical composition comprising the same 失效
标题翻译：二芳基庚酰胺衍生物和包含它们的药物组合物
公开(公告)号：US5763673A
公开(公告)日：1998-06-09
申请号：US561976
申请日：1995-11-22
申请人： Ryuta Yamazaki , Takeshi Matsuzaki , Ritsuo Aiyama , Shusuke Hashimoto , Teruo Yokokura
发明人： Ryuta Yamazaki , Takeshi Matsuzaki , Ritsuo Aiyama , Shusuke Hashimoto , Teruo Yokokura
IPC分类号： C12N9/99 , A61K31/12 , A61P29/00 , A61P43/00 , C07C45/74 , C07C49/255 , C07C49/603
CPC分类号： C07C49/255 , C07C45/74
摘要： A diarylheptanoide derivative of the following formula (1), ##STR1## and a drug composition comprising this compound, such as a 5-lipoxygenase inhibitor, an antiinflammatory agent, and the like. The diarylheptanoide derivative (1) is effective for treating and preventing various inflammatory diseases due to its strong 5-lipoxygenase inhibiting effect.
摘要翻译：下式（1）的二芳基庚酰胺衍生物，IMAGE（1）和包含该化合物的药物组合物，例如5-脂氧合酶抑制剂，抗炎剂等。二芳基庚酰胺衍生物（1）由于其强烈的5-脂氧合酶抑制作用，对于治疗和预防各种炎性疾病是有效的。

2. 发明授权

US5958978A Specific cyclooxygenase 2 inhibitor and anti-inflammatory agent 失效
标题翻译：特异性环氧合酶2抑制剂和抗炎剂
公开(公告)号：US5958978A
公开(公告)日：1999-09-28
申请号：US29738
申请日：1998-03-11
申请人： Ryuta Yamazaki , Takeshi Matsuzaki , Shusuke Hashimoto , Teruo Yokokura
发明人： Ryuta Yamazaki , Takeshi Matsuzaki , Shusuke Hashimoto , Teruo Yokokura
IPC分类号： C12N9/99 , A61K31/195 , A61K31/196 , A61P29/00 , A61P43/00 , C07C229/42 , A61K31/19
CPC分类号： A61K31/196
摘要： The invention relates to a specific cyclooxygenase 2 inhibitor which comprises, as an active ingredient, 2-(2,6-dichloro-4-hydroxyanilino)phenylacetic acid represented by the following formula (1): ##STR1## or a salt thereof, as an anti-inflammatory agent. The compound specifically inhibits cyclooxygenase 2 without inhibiting cyclooxygenase 1 activity and thus it is low in toxicity and safe.
摘要翻译： PCT No.PCT / JP96 / 02583 Sec。 371日期1998年3月11日 102（e）1998年3月11日PCT PCT 1996年9月11日PCT公布。出版物WO97 / 09977 日期：1997年3月20日本发明涉及一种特定的环氧合酶2抑制剂，其包含作为活性成分的由下式（1）表示的2-（2,6-二氯-4-羟基苯胺基）苯乙酸或其盐，作为抗炎剂。该化合物特异性抑制环加氧酶2而不抑制环加氧酶1的活性，因此毒性低，安全。

3. 发明授权

US5601999A Antitumor polysaccharide-glycan complexes 失效
标题翻译：抗肿瘤多糖 - 聚糖复合物
公开(公告)号：US5601999A
公开(公告)日：1997-02-11
申请号：US299414
申请日：1994-09-01
申请人： Takeshi Matsuzaki , Masato Nagaoka , Koji Nomoto , Shusuke Hashimoto , Teruo Yokokura
发明人： Takeshi Matsuzaki , Masato Nagaoka , Koji Nomoto , Shusuke Hashimoto , Teruo Yokokura
IPC分类号： A61K31/715 , A61K35/74 , A61P35/00 , C12P19/04 , C12P19/00
CPC分类号： C12P19/04 , A61K31/715 , A61K35/744 , A61K35/745 , A61K35/747
摘要： An antitumor agent is provided by including, as an active ingredient, a polysaccharide-glycan complex obtained by treating a Gram-positive bacteria such as lactic acid bacteria and Bifidobacterium strains with a cell wall lytic enzyme produced by a bacterium belonging to the genus Achromobacter.The polysaccharide-glycan complex has no toxicity and causes no side effect. Being water-soluble, it is easily formulated into any arbitrary dose form, such as an injectable solution. It can easily be prepared from an easily available starting material.
摘要翻译：提供抗肿瘤剂作为活性成分，通过用属于无色杆菌的细菌产生的细胞壁裂解酶处理革兰氏阳性菌如乳酸菌和双歧杆菌菌株获得的多糖 - 聚糖复合物。多糖 - 聚糖复合物无毒性，不产生副作用。易溶于水，容易配制成任意剂量形式，如可注射溶液。它可以很容易地从容易获得的原料制备。

4. 发明授权

US5475089A Thrombolytic peptide, production thereof, and thrombolytic agent 失效
标题翻译：溶血肽，其制备和溶栓剂
公开(公告)号：US5475089A
公开(公告)日：1995-12-12
申请号：US75545
申请日：1993-06-14
申请人： Osamu Matsuo , Masashi Sakai , Kisaku Shimura , Hiroshi Sansawa , Tsunekazu Watanabe , Tsuneo Matsumoto , Yoshiyuki Shishido , Shusuke Hashimoto , Teruo Yokokura , Masaharu Onoue , Tomoyuki Sako
发明人： Osamu Matsuo , Masashi Sakai , Kisaku Shimura , Hiroshi Sansawa , Tsunekazu Watanabe , Tsuneo Matsumoto , Yoshiyuki Shishido , Shusuke Hashimoto , Teruo Yokokura , Masaharu Onoue , Tomoyuki Sako
IPC分类号： A61K38/46 , C07K14/31 , C12N9/52 , A61K38/43 , C07K14/00
CPC分类号： C07K14/31
摘要： A thrombolytic peptide composed of 136 amino acids residues, which has little problems of antigenicity and is efficacious in only small doses as compared with staphylokinase (SAK). This peptide is obtained by cleaving amino acids or peptides which do not affect the activity of SAK by using a trypsin protease. In particular, SAK-11, which is obtained by cleaving a peptide composed of ten amino acid residues at the N-terminal of SAK, is superior to SAK in the fibrinolysis, plasminogen activation, and fibrin specificity.
摘要翻译： PCT No.PCT / JP91 / 01722 Sec。 371日期：1993年6月14日 102（e）日期1993年6月14日PCT 1991年12月17日PCT公布。出版物WO92 / 11356 日期：1992年7月9日。一种由136个氨基酸残基组成的血栓溶解肽，与葡萄球菌激酶（SAK）相比，其抗原性问题很小，仅有小剂量有效。通过使用胰蛋白酶蛋白酶切割不影响SAK活性的氨基酸或肽来获得该肽。特别地，通过在SAK的N末端切割由10个氨基酸残基构成的肽获得的SAK-11在纤维蛋白溶解，纤溶酶原激活和纤维蛋白特异性方面优于SAK。

5. 发明授权

US5698534A Antiulcer agent and process for preparing the same 失效
标题翻译：抗溃疡剂及其制备方法
公开(公告)号：US5698534A
公开(公告)日：1997-12-16
申请号：US202642
申请日：1994-02-28
申请人： Masato Nagaoka , Shusuke Hashimoto , Tsunekazu Watanabe , Teruo Yokokura
发明人： Masato Nagaoka , Shusuke Hashimoto , Tsunekazu Watanabe , Teruo Yokokura
IPC分类号： A61K31/70 , A61K31/715 , A61P1/04 , C07H3/08 , C08B37/00 , C12P19/06 , C12R1/01
CPC分类号： A61K31/7004 , A61K31/715
摘要： An antiulcer agent effective on prevention of ulceration and acceleration of healing of ulcers and processes for preparing the same are disclosed. The antiulcer agent comprises rhamnan (a homopolysaccharide), rhamnose or a rhamnose oligomer as an active ingredient. Rhamnan is prepared by separating rhamnan sulfate from rhamnan sulfate-containing algae and desulfurating the rhamnan sulfate. Rhamnan oligomers are prepared by hydrolyzing rhamnan obtained by desulfuration of rhamnan sulfate or by hydrolyzing microbial cells of a Bifidobacterium or polysaccharides separated therefrom.
摘要翻译：公开了一种有效预防溃疡溃疡和加速溃疡愈合的抗溃疡剂及其制备方法。抗溃疡剂含有作为活性成分的鼠李糖（均聚多糖），鼠李糖或鼠李糖寡聚物。鼠李糖通过从含有硫酸鼠李糖的藻类中分离出硫酸鼠李糖并且将硫酸鼠李糖硫酸盐脱硫来制备。通过水解通过硫酸鼠李糖硫酸脱硫获得的鼠李糖或通过水解分离的双歧杆菌或多糖的微生物细胞来制备鼠李糖低聚物。

6. 发明授权

US06589937B1 Peptides and nootropic agent 失效
标题翻译：肽和诱导剂
公开(公告)号：US06589937B1
公开(公告)日：2003-07-08
申请号：US09171245
申请日：1998-10-14
申请人： Shuichi Tanabe , Yoshiyuki Shishido , Masayoshi Furushiro , Kunio Kado , Shusuke Hashimoto , Teruo Yokokura , Tetsuya Terasaki
发明人： Shuichi Tanabe , Yoshiyuki Shishido , Masayoshi Furushiro , Kunio Kado , Shusuke Hashimoto , Teruo Yokokura , Tetsuya Terasaki
IPC分类号： A61K3803
CPC分类号： C07K7/16 , A61K38/00 , C07K5/1019
摘要： New peptides represented by the following general formula (wherein X is OH or NH2, R is an amino acid residue selected from Arg, His, Lys, Methyl-Arg or Methyl-Tyr, n is an integer of 1-4, and in the case that n is 2-4, R may be identical with or different from each other) and an anti-dementia drug which contains one or more of these new peptides and has a high blood brain barrier (BBB) permeability and furthermore is low in a side effect.
摘要翻译：由以下通式表示的新肽（其中X为OH或NH 2，R为选自Arg，His，Lys，Methyl-Arg或Methyl-Tyr的氨基酸残基，n为1-4的整数， n为2-4的情况，R可以相同或不同）和含有这些新肽中的一种或多种且具有高血脑屏障（BBB）渗透性的抗痴呆药物，此外，低副作用。

7. 发明授权

US5061800A Camptothecin derivatives 失效
标题翻译： CAMPTOTHECIN衍生物
公开(公告)号：US5061800A
公开(公告)日：1991-10-29
申请号：US298976
申请日：1989-01-19
申请人： Takashi Yaegashi , Satoru Okajima , Seigo Sawada , Kenichiro Nokata , Kenichi Tezuka , Hiroshi Nagata , Teruo Yokokura , Tadashi Miyasaka , Tadashi Miyasaka
发明人： Takashi Yaegashi , Satoru Okajima , Seigo Sawada , Kenichiro Nokata , Kenichi Tezuka , Hiroshi Nagata , Teruo Yokokura , Tadashi Miyasaka , Tadashi Miyasaka
IPC分类号： C07D491/147 , A61K31/47 , A61K31/475 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R.sup.4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R.sup.5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 substituents should not be a hydrogen atom and also that if any one of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.

8. 发明授权

US5843954A Camptothecin derivatives, preparations thereof and antitumor agents 失效
标题翻译：喜树碱衍生物，其制剂和抗肿瘤剂
公开(公告)号：US5843954A
公开(公告)日：1998-12-01
申请号：US976398
申请日：1997-11-21
申请人： Takashi Yaegashi , Seigo Sawada , Tomio Furuta , Teruo Yokokura
发明人： Takashi Yaegashi , Seigo Sawada , Tomio Furuta , Teruo Yokokura
IPC分类号： A61K31/47 , A61K31/4745 , A61P35/00 , C07D209/00 , C07D221/00 , C07D471/14 , C07D487/02
CPC分类号： C07D471/14
摘要： New camptothecin derivatives of the general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen or a C.sub.1 -C.sub.6 alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, C.sub.2 -C.sub.6 acyloxy or methoxyethoxymethoxy group, R.sup.4 represents a hydrogen or halogen atom, and R.sup.5 represents a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 unsaturated alkyl, alkylthioalkyl, alkoxyalkyl, pyridyl or substituted phenyl group, with the proviso that all of the R.sup.2, R.sup.3 and R.sup.4 substituents should not be a hydrogen atom, and a process for preparing the new camptothecin derivatives by subjecting the camptothecin derivatives of the general formula (2): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the same meanings as given above, to the reaction with N,N-dimethylethylenediamine without solvent to open the E-lactone ring followed by acylation of 17-hydroxyl group with corresponding acylating agents and an antitumor agent containing the same as an active ingredient.
摘要翻译：（1）的新喜树碱衍生物：其中R1表示氢原子或C1-C6烷基，R2表示氢或C1-C6烷氧基，R3表示氢或卤素原子或C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，C 2 -C 6酰氧基或甲氧基乙氧基甲氧基，R 4表示氢或卤素原子，R 5表示C 1 -C 6烷基，C 3 -C 6不饱和烷基，烷硫基烷基，烷氧基烷基，吡啶基或取代的苯基，条件是所有的R 2，R 3和R 4取代基不应该是氢原子，以及通过使通式（2）的喜树碱衍生物进行制备来制备新的喜树碱衍生物的方法：（2）其中R 1，R 2，R 3和R 4具有与上述相同的含义，与没有溶剂的N，N-二甲基乙二胺反应以打开E-内酯环，随后用相应的酰化剂酰化17-羟基，含有与活性物质相同的抗肿瘤剂 e成分。

9. 发明授权

US5234904A Antihypertensives containing polysaccharide peptidoglycan complexes extracted from the cell wall of lactic acid bacteria 失效
标题翻译：含有从酸性细菌细胞壁提取的多糖肽肽复合物的抗生素
公开(公告)号：US5234904A
公开(公告)日：1993-08-10
申请号：US542734
申请日：1990-06-22
申请人： Haruji Sawada , Masayoshi Furusiro , Kouichi Hirai , Mahoko Motoike , Tunekazu Watanabe , Teruo Yokokura , Masaaki Watanuki , Seizaburo Kobayashi
发明人： Haruji Sawada , Masayoshi Furusiro , Kouichi Hirai , Mahoko Motoike , Tunekazu Watanabe , Teruo Yokokura , Masaaki Watanuki , Seizaburo Kobayashi
IPC分类号： A23L1/30 , A61K31/00 , A61K35/74 , A61K38/00 , A61P9/00 , A61P9/12 , C07K9/00
CPC分类号： C07K9/005 , A23C9/123 , A23L2/382 , A23L33/18 , A61K31/715 , A61K38/164 , A23V2002/00
摘要： The present invention relates to antihypertensives and food and drinks, containing as effective component polysaccharideglycopeptide complexes derived from cell wall of Gram positive bacteria (also referred to as peptidoglycan). The present invention provides extremely strong and safe antihypertensives and food and drinks, which may exert hypotensive effects if administered orally to spontaneous hypertensive rats and renal hypertensive rats at a single dose as low as 1 mg/kg.

10. 发明授权

US4347240A Antitumor agent containing Lactobacillus casei YIT 9018 失效
标题翻译：含有干酪乳杆菌YIT 9018的抗肿瘤剂
公开(公告)号：US4347240A
公开(公告)日：1982-08-31
申请号：US124725
申请日：1980-02-26
申请人： Masahiko Mutai , Teruo Yokokura , Seizaburo Kobayashi , Ikuo Kato
发明人： Masahiko Mutai , Teruo Yokokura , Seizaburo Kobayashi , Ikuo Kato
IPC分类号： C12N1/20 , A61K35/74 , A61P35/00 , A61K39/02
CPC分类号： C12R1/245 , A61K35/747
摘要： Immunostimulating agent for inhibiting tumors comprising Lactobacillus casei YIT 9018 and methods for treating and/or preventing tumor growth.
摘要翻译：用于抑制肿瘤的免疫刺激剂，其包含干酪乳杆菌YIT 9018以及用于治疗和/或预防肿瘤生长的方法。

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