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1. 发明授权

US5863907A Carboxymethylmannoglucans and derivatives thereof 失效
公开(公告)号：US5863907A
公开(公告)日：1999-01-26
申请号：US681981
申请日：1996-07-30
申请人： Kazuhiro Inoue , Teruomi Ito , Takayuki Kawaguchi , Katsutoshi Aono , Satoshi Okuno , Toshiro Yano
发明人： Kazuhiro Inoue , Teruomi Ito , Takayuki Kawaguchi , Katsutoshi Aono , Satoshi Okuno , Toshiro Yano
IPC分类号： A61K47/36 , A61K47/48 , C08B15/00 , C08B37/00 , A61K31/725 , A61K31/715 , A61K31/72
CPC分类号： C08B37/0087 , A61K47/4823
摘要： A carboxymethylmannoglucan comprising tetrasaccharide units represented by the following general formula (I) and salt thereof. Further, the invention discloses a carboxymethylmannoglucan derivative and salt thereof produced by subjecting part or the whole of mannose of the tetrasaccharide units to ring opening and subjecting part or the whole of glucose which constitute the main chain but have no mannose as a branch ##STR1## wherein R.sup.1 to R.sup.12 each represent a hydrogen atom or a carboxymethyl group.The compounds are useful as carrier for delaying the disappearance of a drug in the blood and for enhancing the organotropism of the drug for a carcinoma.

2. 发明授权

US5463022A N-acetylcarboxymethylchitosan derivatives and process for preparation thereof 失效
公开(公告)号：US5463022A
公开(公告)日：1995-10-31
申请号：US969307
申请日：1993-02-16
申请人： Kazuhiro Inoue , Teruomi Ito , Satoshi Okuno , Katsutoshi Aono
发明人： Kazuhiro Inoue , Teruomi Ito , Satoshi Okuno , Katsutoshi Aono
IPC分类号： A61K47/48 , C08B37/08 , A61K38/00 , C07G17/00 , C07K9/00 , C08B37/00
CPC分类号： C08B37/003
摘要： N-acetylcarboxymethylchitosan derivatives are provided by the present invention. They are represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 individually mean H or carboxymethyl group; P denotes a group R.sub.3 CO--, a group R.sub.4 NH-- or a group R.sub.5 O-- with assuming that R.sub.3 COOH denotes a compound having carboxyl group, R.sub.4 NH.sub.2 denotes a compound having amino group and R.sub.5 OH denotes an alcohol compound; Q stands for H or a group --OH; X represents a peptide chain containing same or different, one to ten amino acids; a.sub.1 and a.sub.2 individually represent zero or a positive integer, provided that both of a.sub.1 and a.sub.2 are not zero at the same time, and b stands for a positive integer; and having the following characteristic values (1)-(4):______________________________________ (1) carboxymethylation degree: 0.5-1.2 (2) molecular weight (as measured 3,000-300,000 by gel filtration method): (3) a/(a + b): 0.01-1 [provided that a = a.sub.1 + a.sub.2 ] (4) P/X ratio (molar ratio): 0.1-1 ______________________________________ P in the formula (I) can be the residue of a pharmaceutical compound. In this case, the substances of the formula (I) are derivatives of the pharmaceutical compound, which derivatives have been improved in the properties such as organotropism in vivo.P in the formula (I) can also be protective groups. In this case, removal of the protective groups from the substances of the formula (I) by deprotection makes it possible to provide such N-acetylcarboxymethylchitosan derivative which is useful as carrier for pharmaceutical compounds and which has the terminals of the so deprotected peptide chains capable of being linked with a pharmaceutical compound.There are further obtained such derivatives of the substances of the formula (I), in which derivatives some of the N-acetylcarboxymethylglucosamine units have been replaced by units having a high solubility in water.

3. 发明授权

US5863908A Carboxymethylmannoglucans and derivatives thereof 失效
标题翻译：羧甲基甘露糖葡聚糖及其衍生物
公开(公告)号：US5863908A
公开(公告)日：1999-01-26
申请号：US689095
申请日：1996-07-30
申请人： Kazuhiro Inoue , Teruomi Ito , Takayuki Kawaguchi , Katsutoshi Aono , Satoshi Okuno , Toshiro Yano
发明人： Kazuhiro Inoue , Teruomi Ito , Takayuki Kawaguchi , Katsutoshi Aono , Satoshi Okuno , Toshiro Yano
IPC分类号： A61K47/36 , A61K47/48 , C08B15/00 , C08B37/00 , A61K31/725 , A61K31/715 , A61K31/72
CPC分类号： C08B37/0087 , A61K47/4823
摘要： A carboxymethylmannoglucan comprising tetrasaccharide units represented by the following general formula (I) and salt thereof. Further, the invention discloses a carboxymethylmannoglucan derivative and salt thereof produced by subjecting part or the whole of mannose of the tetrasaccharide units to ring opening and subjecting part or the whole of glucose which constitute the main chain but have no mannose as a branch ##STR1## wherein R.sup.1 to R.sup.12 each represent a hydrogen atom or a carboxymethyl group.The compounds are useful as carrier for delaying the disappearance of a drug in the blood and for enhancing the organotropism of the drug for a carcinoma.
摘要翻译：包含由以下通式（I）表示的四糖单元及其盐的羧甲基甘露糖葡聚糖。此外，本发明公开了通过使四糖单元的一部分或全部甘露糖开环并使构成主链但不具有甘露糖的部分或全部葡萄糖作为分支而制备的羧甲基葡萄糖聚糖衍生物及其盐。（I）其中R 1至R 12各自表示氢原子或羧甲基。这些化合物可用作延迟药物在血液中消失并用于增强癌症药物的有机性的载体。

4. 发明授权

US5567690A Carboxymethylmannoglucans and derivatives thereof 失效
公开(公告)号：US5567690A
公开(公告)日：1996-10-22
申请号：US397560
申请日：1995-03-02
申请人： Kazuhiro Inoue , Teruomi Ito , Takayuki Kawaguchi , Katsutoshi Aono , Satoshi Okuno , Toshiro Yano
发明人： Kazuhiro Inoue , Teruomi Ito , Takayuki Kawaguchi , Katsutoshi Aono , Satoshi Okuno , Toshiro Yano
IPC分类号： A61K47/36 , A61K47/48 , C08B15/00 , C08B37/00 , A61K31/725 , A61K31/715 , A61K31/72
CPC分类号： C08B37/0087 , A61K47/4823
摘要： A carboxymethylmannoglucan comprising tetrasaccharide units represented by the following general formula (I) and salt thereof. Further, the invention discloses a carboxymethylmannoglucan derivative and salt thereof produced by subjecting part or the whole of mannose of the tetrasaccharide units to ring opening and subjecting part or the whole of glucose which constitute the main chain but have no mannose as a branch ##STR1## wherein R.sup.1 to R.sup.12 each represent a hydrogen atom or a carboxymethyl group.The compounds are useful as carrier for delaying the disappearance of a drug in the blood and for enhancing the organotropism of the drug for a carcinoma.

5. 发明授权

US4577038A Glycolic acid type platinum complexes 失效
标题翻译：乙醇酸型铂络合物
公开(公告)号：US4577038A
公开(公告)日：1986-03-18
申请号：US606961
申请日：1984-05-04
申请人： Tetsushi Totani , Katsutoshi Aono
发明人： Tetsushi Totani , Katsutoshi Aono
IPC分类号： A61K31/28 , A61P35/00 , C07F15/00
CPC分类号： C07F15/0093
摘要： Novel platinum complexes of glycolic acid type having potent antitumor activity and high water solubility with low nephrotoxicity and a pharmaceutical composition containing one or more said compounds together with one or more carriers, diluents or excipients are provided. They can be administered parenterally to patients suffering from malignant tumors.They are prepared by passing nitrato-platinum complexes of amines through anion exchange resins and subsequent reaction with glycolic acids.
摘要翻译：提供具有有效抗肿瘤活性和低肾毒性高水溶性的乙醇酸型新型铂络合物和含有一种或多种所述化合物与一种或多种载体，稀释剂或赋形剂的药物组合物。它们可以肠胃外给予恶性肿瘤患者。它们通过使胺的硝化铂络合物通过阴离子交换树脂并随后与乙醇酸反应来制备。

6. 发明授权

US4902797A Ammine-alicyclic amine-platinum complexes and antitumor agents 失效
标题翻译：氨 - 脂环胺 - 铂络合物和抗肿瘤剂
公开(公告)号：US4902797A
公开(公告)日：1990-02-20
申请号：US135061
申请日：1987-12-18
申请人： Tetsushi Totani , Katsutoshi Aono , Yasuko Adachi
发明人： Tetsushi Totani , Katsutoshi Aono , Yasuko Adachi
IPC分类号： C07F17/02 , A61K31/555 , C07F15/00
CPC分类号： C07F15/0093
摘要： A compound of the formula (I): ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, hydroxy, carboxy, C.sub.1 -C.sub.6 alkoxy, halogen or oxo; m is an integer from 2 to 7; X and Y each is chlorine or nit-rato ligand, or taken together form --OCOCH(R.sup.1)O--, OCOCOO--, ##STR2## R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, hydroxymethyl, halogmethyl or phenyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.5 alkyl; and n is an integer from 2 to 5), being useful as antitumor agents is provided.

7. 发明授权

US06765096B1 Tricyclic compound having acyloxymethoxycarbonyl side chain 失效
标题翻译：具有酰氧基甲氧基羰基侧链的三环化合物
公开(公告)号：US06765096B1
公开(公告)日：2004-07-20
申请号：US09980474
申请日：2001-12-03
申请人： Katsutoshi Aono , Teruhisa Ichinashi , Akira Kugimiya
发明人： Katsutoshi Aono , Teruhisa Ichinashi , Akira Kugimiya
IPC分类号： C07D21363
CPC分类号： C07D213/70 , A61K31/136 , A61K31/4418 , C07D213/64 , C07D213/74 , C07D213/75 , C07D213/77 , C07D239/26 , C07D239/34
摘要： There are provided a compound represented by the formula (I): wherein X and X′ are —N(COOCR3R2OCOR1)—, —O— or the like, R1 is alkyl substituted with carbamoyl, lower alkylcarbamoyl, carbamoyloxy, lower alkylcarbamoyloxy, acetylamino or the like, R2 and R3 are hydrogen or the like, Y and Y′ are lower alkyl, lower alkenyl or the like, ring A, ring B and ring C are optionally substituted aromatic carbocycle or optionally substituted heterocycle, W1, W2 and/or W3 are a bond or the like, and V1 and V2 are a single bond or the like, or a pharmaceutically acceptable salt or a solvate thereof, as well as a pharmaceutical composition containing the present compound.
摘要翻译：提供由式（I）表示的化合物：其中X和X'是-N（COOCR 3 R 2 OCOR 1） - ， - O-等，R 1是烷基被氨基甲酰基，低级烷基氨基甲酰基，氨基甲酰氧基，低级烷基氨基甲酰氧基，乙酰氨基等取代，R 2和R 3为氢等，Y和Y'为低级烷基，低级烯基等，环A，环 B和环C是任选取代的芳族碳环或任选取代的杂环，W 1，W 2和/或W 3是键或类似的，V 1和V 2是单键或其药学上可接受的盐或溶剂合物，以及含有本发明化合物的药物组合物。

8. 发明授权

US4560781A Glycolic acid platinum complexes 失效
标题翻译：乙醇酸铂络合物
公开(公告)号：US4560781A
公开(公告)日：1985-12-24
申请号：US552906
申请日：1983-11-17
申请人： Tetsushi Totani , Katsutoshi Aono , Michihiro Komura
发明人： Tetsushi Totani , Katsutoshi Aono , Michihiro Komura
IPC分类号： C07F17/02 , A61K31/28 , A61P35/00 , C07C51/41 , C07C59/06 , C07C211/65 , C07F15/00
CPC分类号： C07F15/0093 , C07C51/418 , C07C59/06
摘要： Novel water-soluble glycolic acid platinum complexes which have more potent antitumor activity with lower nephrotoxicity than cisplatin are provided.They can be administered parenterally to mice attacked by malignant tumors.Prepared from dinitrato-platinum complexes of amines on treatment with anion exchange resins and subsequent reaction with glycolic acid.
摘要翻译：提供了具有比顺铂更低的肾毒性的更有效的抗肿瘤活性的新型水溶性乙醇酸铂络合物。它们可以肠胃外给予恶性肿瘤侵袭的小鼠。由胺的二硝基铂络合物制备，用阴离子交换树脂处理，随后与乙醇酸反应。

9. 发明授权

US6054591A Lymph-absorbable aryl substituted imidazole derivatives 失效
标题翻译：可吸收吸收的芳基取代咪唑衍生物
公开(公告)号：US6054591A
公开(公告)日：2000-04-25
申请号：US101960
申请日：1998-07-21
申请人： Katsutoshi Aono , Teruhisa Ichihashi , Tamio Sugawara , Koichiro Hirano
发明人： Katsutoshi Aono , Teruhisa Ichihashi , Tamio Sugawara , Koichiro Hirano
IPC分类号： A61K31/415 , C07D233/58 , C07D233/84 , C07D401/06
CPC分类号： C07D401/06 , A61K31/415 , C07D233/84
摘要： A compound of the formula (I): ##STR1## salt thereof, or hydrate thereof which can effectively be absorbed from the lymph vessel in the intestinal tract and transferred to the lymph node in a high concentration is provided.
摘要翻译： PCT No.PCT / JP97 / 00813 Sec。 371日期：1998年7月21日 102（e）1998年7月21日PCT PCT 1997年3月14日PCT公布。公开号WO97 / 35843 日期1997年10月2日提供了可以有效地从肠道中的淋巴管吸收并以高浓度转移到淋巴结的式（I）化合物：其盐或其水合物。

10. 发明授权

US4658048A Platinum complexes 失效
标题翻译：铂金复合体
公开(公告)号：US4658048A
公开(公告)日：1987-04-14
申请号：US741890
申请日：1985-06-06
申请人： Tetsushi Totani , Osamu Shiratori , Katsutoshi Aono , Naomi Uchida
发明人： Tetsushi Totani , Osamu Shiratori , Katsutoshi Aono , Naomi Uchida
IPC分类号： A61K31/555 , A61P35/00 , C07F15/00 , C07F17/02 , A01N55/02 , A61K31/28
CPC分类号： C07F15/0093
摘要： Novel platinum (IV) complexes having potent antitumor and antibacterial activities and high water solubility with low toxicity and pharmaceutical and/or veterinarily compositions containing one or more compounds together with one or more carriers are provided.They can be prepared by reacting a corresponding platinum (II) complex with hydrogen peroxide or halogen.
摘要翻译：提供了具有有效的抗肿瘤和抗菌活性和低毒性的高水溶性和具有一种或多种化合物以及一种或多种载体的药物和/或兽用组合物的新型铂（IV）配合物。它们可以通过使相应的铂（II）络合物与过氧化氢或卤素反应来制备。

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