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公开(公告)号：US5410024A
公开(公告)日：1995-04-25
申请号：US6465
申请日：1993-01-21
申请人： George R. Pettit , Jozsef Barkoczy , Darko Kantoci
发明人： George R. Pettit , Jozsef Barkoczy , Darko Kantoci
CPC分类号： C07K5/0205 , A61K38/00 , Y02P20/55
摘要： The synthesis of useful peptides presents a promising approach to new theeutic agents. The Dolastatins, a series of linear and cyclic antineoplastic and/or cytostatic peptides isolated from Indian Ocean sea hare Dolabella auricularia represent excellent leads for synthetic modification.The extraordinary inhibition of cell growth shown by the pentapeptideamides against six major types of human cancer has been presented. The intermediates of these reaction also show anticancer activity against the murine P388 lymphocytic leukemia cell line.
摘要翻译： 有用的肽的合成为新的治疗剂提供了有希望的方法。 Dolastatins，一系列线性和环状抗肿瘤和/或细胞生长抑制肽，分离自印度洋海洋，海豚耳朵，代表了合成改性的优秀引线。 已经提出了五肽对六种主要类型的人类癌症表现出的细胞生长的非凡抑制作用。 这些反应的中间体也显示对鼠P388淋巴细胞白血病细胞系的抗癌活性。
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公开(公告)号：US5663149A
公开(公告)日：1997-09-02
申请号：US354551
申请日：1994-12-13
摘要： The synthesis and elucidation of nineteen heterocyclic or halophenyl amideerivatives of dolastatin 10 are disclosed. These compounds and the methods of producing those compounds offer demonstrated significant in vitro activity against several human cancer cell lines. These compounds and the methods of producing those compounds offer a commercially viable alternative to natural and synthetic dolastatin 10.
摘要翻译： 公开了多拉司他汀10的十九种杂环或卤代苯基酰胺衍生物的合成和说明。 这些化合物和生产这些化合物的方法证明了对几种人类癌细胞系的显着的体外活性。 这些化合物和生产这些化合物的方法提供商业可行的天然和合成多拉司他汀10的替代物。
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公开(公告)号：US6083982A
公开(公告)日：2000-07-04
申请号：US57731
申请日：1998-04-09
IPC分类号： C07D333/58 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/39 , A61P7/10 , B01J31/02 , C07B61/00 , C07C51/09 , C07C59/52 , C07C59/84 , C07C59/90 , C07C61/29 , C07C61/39 , C07C61/40 , C07C62/32 , C07C62/34 , C07C67/343 , C07C69/732 , C07C69/738 , C07C69/76 , C07C211/26 , C07C211/29 , C07C211/34 , C07C211/37 , C07C211/44 , C07C231/24 , C07C233/11 , C07C235/32 , C07C235/78 , C07C317/32 , C07C317/44 , C07D307/33 , C07D311/58 , C07D311/72 , C07D333/60 , C07D333/64 , C07D335/06 , C07D337/08 , C07D337/16 , C07D493/04 , G11C11/407 , G11C16/02 , G11C29/14 , A61K31/215 , A61K31/19 , A61K31/235
CPC分类号： C07D307/33 , A61K31/353 , A61K31/365 , C07C59/90 , C07C69/732 , C07C69/738 , C07D311/72 , C07D493/04
摘要： Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolonged potassium excretion.
摘要翻译： 化合物，方法和组合物用于在哺乳动物中诱导利尿。 还提供了分离和合成利尿钠化合物的方法。 还提供了使用利尿钠化合物的治疗方法。 利钠化合物能够在哺乳动物中诱导钠排泄，而不引起相应的延长的钾排泄。
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4.发明授权Adamantyl comprising tripeptides, derivatives and hydrochlorides thereof, their preparation and use 失效包含其中的三聚体，衍生物和盐酸盐，其制备和使用
公开(公告)号：US5066642A
公开(公告)日：1991-11-19
申请号：US477373
申请日：1990-02-09
申请人： Branka Vranesic , Jelka Tomasic , Stanislav Smerdel , Darko Kantoci , Gianni Sava , Ivo Hrsak
发明人： Branka Vranesic , Jelka Tomasic , Stanislav Smerdel , Darko Kantoci , Gianni Sava , Ivo Hrsak
CPC分类号： C07K5/0812 , A61K38/00 , Y10S514/934
摘要： 2-Adamantyl- and 1-adamantyl-D/L-glycyl-L-alanyl-D-isoglutamine and their derivatives of the formulae ##STR1## wherein R stands for a hydrogen atom or a MurNAc group, and hydrochlorides thereof,a process for the preparation thereof and their use to obtain pharmaceuticals, which are particularly indicated for the treatment of viral diseases and tumors and/or immunomodulations in humans and animals.
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公开(公告)号：US6150402A
公开(公告)日：2000-11-21
申请号：US290430
申请日：1994-08-15
IPC分类号： C07D333/58 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/39 , A61P7/10 , B01J31/02 , C07B61/00 , C07C51/09 , C07C59/52 , C07C59/84 , C07C59/90 , C07C61/29 , C07C61/39 , C07C61/40 , C07C62/32 , C07C62/34 , C07C67/343 , C07C69/732 , C07C69/738 , C07C69/76 , C07C211/26 , C07C211/29 , C07C211/34 , C07C211/37 , C07C211/44 , C07C231/24 , C07C233/11 , C07C235/32 , C07C235/78 , C07C317/32 , C07C317/44 , C07D307/33 , C07D311/58 , C07D311/72 , C07D333/60 , C07D333/64 , C07D335/06 , C07D337/08 , C07D337/16 , C07D493/04 , G11C11/407 , G11C16/02 , G11C29/14 , A61K31/355
CPC分类号： C07D307/33 , A61K31/353 , A61K31/365 , C07C59/90 , C07C69/732 , C07C69/738 , C07D311/72 , C07D493/04
摘要： Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolongated potassium excretion.
摘要翻译： 化合物，方法和组合物用于在哺乳动物中诱导利尿。 还提供了分离和合成利尿钠化合物的方法。 还提供了使用利尿钠化合物的治疗方法。 利钠化合物能够在哺乳动物中诱导钠排泄，而不诱导相应的延长的钾排泄。
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公开(公告)号：US5846967A
公开(公告)日：1998-12-08
申请号：US822046
申请日：1997-03-24
IPC分类号： A61K31/55 , A61K31/554 , A61P1/16 , A61P7/10 , A61P9/00 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , C07D281/10
CPC分类号： C07D281/10
摘要： A compound having the formula I ##STR1## in which R.sub.1, R.sub.2 independently are OH, OOC--R.sub.3 or O--R.sub.3, and R.sub.3 is an unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, alkenyl, alkynyl or phenyl group. The compound is useful as a natriuretic and anti-hypertensive agent.
摘要翻译： 具有式I
的化合物，其中R1，R2独立地是OH，OOC-R3或O-R3，R3是未取代或取代的C1-C6烷基，烯基，炔基或苯基。 该化合物可用作利尿钠和抗高血压药。 -
7.发明授权New adamantyl comprising tripeptides, derivatives and hydrochlorides thereof, their preparation and use 失效包括三肽，其衍生物和盐酸盐的新金刚烷，其制备和用途
公开(公告)号：US5286715A
公开(公告)日：1994-02-15
申请号：US792619
申请日：1991-11-15
申请人： Branka Vranesic , Jelka Tomasic , Stanislay Smerdel , Darko Kantoci , Gianni Sava , Ivo Hrsak
发明人： Branka Vranesic , Jelka Tomasic , Stanislay Smerdel , Darko Kantoci , Gianni Sava , Ivo Hrsak
CPC分类号： C07K5/0812 , A61K38/00 , Y10S514/934
摘要： 2-Adamantyl- and 1-adamantyl-D/L-glycyl-L-alanyl-D-isoglutamine and their derivatives of the formulae ##STR1## wherein R stands for a hydrogen atom or a MurNAc group, and hydrochlorides thereof, a process for the preparation thereof and their use to obtain pharmaceuticals, which are particularly indicated for the treatment of viral diseases and tumors and/or immunomodulations in humans and animals.
摘要翻译： 2-金刚烷基和1-金刚烷基-D / L-甘氨酰-L-丙氨酰-D-异谷氨酰胺及其衍生物（*化学结构*）（Ia）（*化学结构*）（Ib）其中R代表 氢原子或MurNAc基团，其盐酸盐，其制备方法及其用于获得药物的用途，其特别用于治疗人和动物中病毒性疾病和肿瘤和/或免疫调节。
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