专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5677470A Baccatin derivatives and processes for preparing the same 失效
标题翻译：浆果赤霉素衍生物及其制备方法
公开(公告)号：US5677470A
公开(公告)日：1997-10-14
申请号：US480052
申请日：1995-06-07
申请人： Kenji Tsujihara , Tomiki Hashiyama , Naoyuki Harada , Kunihiko Ozaki , Motoaki Ohashi , Noriyuki Nakanishi , Tetsuo Yamaguchi
发明人： Kenji Tsujihara , Tomiki Hashiyama , Naoyuki Harada , Kunihiko Ozaki , Motoaki Ohashi , Noriyuki Nakanishi , Tetsuo Yamaguchi
IPC分类号： C07D305/14 , C07D407/12 , C07D409/12
CPC分类号： C07D407/12 , A61K47/48038 , C07D305/14 , C07D409/12 , Y02P20/55
摘要： Disclosed are 13.alpha.-(3-substituted-2-hydroxypropionyloxy)baccatin compounds represented by the formula: ##STR1## wherein R.sup.1 represents a lower alkanoyl group or a protective group for hydroxy group; R.sup.2 represents a protective group for hydroxy group; R.sup.3 represents a lower alkanoyl group; R.sup.4 represents a substituted or unsubstituted benzoyl group; X represents a substituted or unsubstituted aryl group, a substituted or unsubstituted lower alkenyl group, or a substituted or unsubstituted lower alkynyl group; and A' represents a halogen atom, azido group or amino group, and processes for preparing the same.
摘要翻译：公开了由下式表示的13α-（3-取代-2-羟基丙酰氧基）浆果赤霉素化合物：其中R1代表低级烷酰基或羟基保护基; R2表示羟基的保护基; R3表示低级烷酰基; R4表示取代或未取代的苯甲酰基; X表示取代或未取代的芳基，取代或未取代的低级烯基或取代或未取代的低级炔基; A'表示卤素原子，叠氮基或氨基，及其制备方法。

2. 发明授权

US5589502A Baccatin derivatives and processes for preparing the same 失效
标题翻译：浆果赤霉素衍生物及其制备方法
公开(公告)号：US5589502A
公开(公告)日：1996-12-31
申请号：US558772
申请日：1995-11-15
申请人： Kenji Tsujihara , Tomiki Hashiyama , Motoaki Ohashi , Noriyuki Nakanishi
发明人： Kenji Tsujihara , Tomiki Hashiyama , Motoaki Ohashi , Noriyuki Nakanishi
IPC分类号： C07D263/04 , C07D263/06 , C07D305/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K31/335
CPC分类号： C07D263/04 , C07D263/06 , C07D305/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12
摘要： A compound represented by the formula [I]: ##STR1## wherein R.sup.3 represents a lower alkanoyl group; R.sup.4 represents a substituted or unsubstituted benzoyl group; ring A represents a substituted or unsubstituted cyclopropane ring; X represents a single bond or a group represented by --O--, --S-- or --NH--; R represents a substituted or unsubstituted lower alkyl group (wherein said lower alkyl group may have a cycloalkyl moiety), a substituted or unsubstituted aryl group or a substituted or unsubstituted aromatic heterocyclic group; E represents hydrogen atom or a group represented by --CO(CH.sub.2).sub.n ZY; Y represents a residue obtained from an amino acid or a dipeptide by removing hydroxyl group in one carboxyl group therefrom (wherein amino group existing in said residue may be protected, and carboxyl group existing in said residue may be esterified or amidated); Z represents a group represented by the formula of --O-- or --NH--; and n represents 1, 2, 3, 4, 5 or 6, or a pharmaceutically acceptable salt thereof. Said compounds have excellent antitumor activity so that they are useful in the prophylaxis or treatment of a wide range of tumors such as breast cancer, ovary cancer, lung cancer, malignant melanoma and the like.
摘要翻译：由式[I]表示的化合物：其中R 3表示低级烷酰基; R4表示取代或未取代的苯甲酰基; 环A表示取代或未取代的环丙烷环; X表示单键或由-O - ， - S-或-NH-表示的基团; R表示取代或未取代的低级烷基（其中所述低级烷基可以具有环烷基部分），取代或未取代的芳基或取代或未取代的芳族杂环基; E表示氢原子或由-CO（CH 2）n ZY表示的基团; Y表示通过从其中除去一个羧基中的羟基从氨基酸或二肽获得的残基（其中存在于所述残基中的氨基可被保护，并且所述残基中存在的羧基可被酯化或酰胺化）; Z表示由式-O-或-NH-表示的基团; 和n表示1,2,3,4,5或6或其药学上可接受的盐。所述化合物具有优异的抗肿瘤活性，因此它们可用于预防或治疗广泛范围的肿瘤如乳腺癌，卵巢癌，肺癌，恶性黑素瘤等。

3. 发明授权

US5608073A Baccatin derivatives and processes for preparing the same 失效
标题翻译：浆果赤霉素衍生物及其制备方法
公开(公告)号：US5608073A
公开(公告)日：1997-03-04
申请号：US673580
申请日：1996-07-01
申请人： Kenji Tsujihara , Tomiki Hashiyama , Motoaki Ohashi , Noriyuki Nakanishi
发明人： Kenji Tsujihara , Tomiki Hashiyama , Motoaki Ohashi , Noriyuki Nakanishi
IPC分类号： C07D263/04 , C07D263/06 , C07D305/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12
CPC分类号： C07D263/04 , C07D263/06 , C07D305/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12
摘要： A compound represented by the formula [I]: ##STR1## wherein R.sup.3 represents a lower alkanoyl group; R.sup.4 represents a substituted or unsubstituted benzoyl group; ring A represents a substituted or unsubstituted cyclopropane ring; X represents a single bond or a group represented by --O--,--S-- or --NH--, R represents a substituted or unsubstituted lower alkyl group (wherein said lower alkyl group may have a cycloalkyl moiety), a substituted or unsubstituted aryl group or a substituted or unsubstituted aromatic heterocyclic group; E represents hydrogen atom or a group represented by --CO(CH.sub.2).sub.n ZY; Y represents a residue obtained from an amino acid or a dipeptide by removing hydroxyl group in one carboxyl group therefrom (wherein amino group existing in said residue may be protected, and carboxyl group existing in said residue may be esterified or amidated); Z represents a group represented by the formula of --O-- or --NH--; and n represents 1, 2, 3, 4, 5 or 6, or a pharmaceutically acceptable salt thereof. Said compounds have excellent antitumor activity so that they are useful in the prophylaxis or treatment of a wide range of tumors such as breast cancer, ovary cancer, lung cancer, malignant melanoma and the like.
摘要翻译：由式[I]表示的化合物：其中R 3表示低级烷酰基; R4表示取代或未取代的苯甲酰基; 环A表示取代或未取代的环丙烷环; X表示单键或由-O - ， - S-或-NH-表示的基团，R表示取代或未取代的低级烷基（其中所述低级烷基可具有环烷基部分），取代或未取代的芳基或取代或未取代的芳族杂环基; E表示氢原子或由-CO（CH 2）n ZY表示的基团; Y表示通过从其中除去一个羧基中的羟基从氨基酸或二肽获得的残基（其中存在于所述残基中的氨基可被保护，并且所述残基中存在的羧基可被酯化或酰胺化）; Z表示由式-O-或-NH-表示的基团; 和n表示1,2,3,4,5或6或其药学上可接受的盐。所述化合物具有优异的抗肿瘤活性，因此它们可用于预防或治疗广泛范围的肿瘤如乳腺癌，卵巢癌，肺癌，恶性黑素瘤等。

4. 发明授权

US5605904A Ellipticine derivative and process for preparing the same 失效
标题翻译：椭圆衍生物及其制备方法
公开(公告)号：US5605904A
公开(公告)日：1997-02-25
申请号：US449273
申请日：1995-05-24
申请人： Kenji Tsujihara , Naoyuki Harada , Kunihiko Ozaki , Motoaki Ohashi , Koji Oda
发明人： Kenji Tsujihara , Naoyuki Harada , Kunihiko Ozaki , Motoaki Ohashi , Koji Oda
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： An ellipticine derivative of the formula [I]: ##STR1## wherein R is a substituted lower alkyl group, a substituted or unsubstituted lower alkoxy group or a heteromonocyclic group, or a pharmaceutically acceptable salt thereof, which show excellent antitumor activity, less side effects, less toxicity and/or high solubility in water and are useful as antitumor agent, and a process for preparing the same.
摘要翻译：式[I]的玫瑰树碱衍生物：其中R是取代的低级烷基，取代或未取代的低级烷氧基或杂单环基或其药学上可接受的盐，其显示出优异的抗肿瘤活性，较少的副作用，较少的毒性和/或在水中的高溶解性，并且可用作抗肿瘤剂，及其制备方法。

5. 发明授权

US5565569A Ellipticine derivative and process for preparing the same 失效
标题翻译：椭圆衍生物及其制备方法
公开(公告)号：US5565569A
公开(公告)日：1996-10-15
申请号：US186016
申请日：1994-01-25
申请人： Kenji Tsujihara , Naoyuki Harada , Kunihiko Ozaki , Motoaki Ohashi , Koji Oda
发明人： Kenji Tsujihara , Naoyuki Harada , Kunihiko Ozaki , Motoaki Ohashi , Koji Oda
IPC分类号： C07D471/04 , A61K31/475
CPC分类号： C07D471/04
摘要： An ellipticine derivative of the formula [I]: ##STR1## wherein R is a substituted lower alkyl group, a substituted or unsubstituted lower alkoxy group or a heteromonocyclic group,or a pharmaceutically acceptable salt thereof, which show excellent antitumor activity, less side effects, less toxicity and/or high solubility in water and are useful as antitumor agent, and a process for preparing the same.
摘要翻译：式[I]的玫瑰树碱衍生物：其中R是取代的低级烷基，取代或未取代的低级烷氧基或杂单环基或其药学上可接受的盐，其显示出优异的抗肿瘤活性，较少的副作用，较少的毒性和/或在水中的高溶解性，并且可用作抗肿瘤剂，及其制备方法。

6. 发明授权

US5650172A Pharmaceutical preparation comprising fat emulsion of fat microparticles 失效
标题翻译：包含脂肪微粒脂肪乳剂的药物制剂
公开(公告)号：US5650172A
公开(公告)日：1997-07-22
申请号：US479143
申请日：1995-06-07
申请人： Saburo Matsuda , Shigeyuki Ishikawa , Akira Suzuki , Kenji Tsujihara , Motoaki Ohashi
发明人： Saburo Matsuda , Shigeyuki Ishikawa , Akira Suzuki , Kenji Tsujihara , Motoaki Ohashi
IPC分类号： A61K9/107 , A61K9/14 , A61K9/19 , A61K47/12 , A61K47/18 , A61K47/26 , A61K9/10 , A61K9/16
CPC分类号： A61K9/14 , A61K9/1075 , A61K9/19 , Y10S514/937 , Y10S514/938
摘要： A preparation comprising a fat emulsion of fat microparticles wherein said emulsion contains a stabilizer consisting essentially of a fatty acid, a basic amino acid and a saccharide is provided. In the preparation comprising a fat emulsion of fat microparticles of the present invention, said microparticles having a mean particle diameter of at most 100 nm are stable, and so the microparticles remain in blood without being uptaken by liver. Therefore in case of administering a pharmaceutical preparation prepared by using the above-mentioned preparation of the present invention, the pharmacological activity may be expressed at a desired site. Thus the preparation is extremely useful as a drug carrier for drug delivery system. Furthermore, the pharmaceutical preparation of the present invention which is lyophilized can be easily and rapidly reconstituted into the pharmaceutical preparation comprising a fat emulsion of stable fat microparticles having a mean particle diameter of about at most 100 nm by adding distilled water, even after a long-term storage.
摘要翻译：提供了包含脂肪微粒的脂肪乳液的制剂，其中所述乳液含有基本上由脂肪酸，碱性氨基酸和糖组成的稳定剂。在包含本发明的脂肪微粒的脂肪乳剂的制剂中，平均粒径为100nm以下的微粒是稳定的，因此微粒保留在血液中而不被肝吸收。因此，在施用通过使用本发明的上述制剂制备的药物的情况下，可以在期望的部位表达药理活性。因此，该制剂作为药物递送系统的药物载体非常有用。此外，冻干的本发明的药物制剂可以通过添加蒸馏水容易且迅速地重构成包含平均粒径为大约100nm的稳定脂肪微粒的脂肪乳剂的药物制剂，即使经过长时间 -term存储。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式