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公开(公告)号:US20100179304A1
公开(公告)日:2010-07-15
申请号:US12587452
申请日:2009-10-07
IPC分类号: C07K1/113 , C07D457/12 , C07D457/06 , C07D457/02
CPC分类号: C07D471/04 , A61K38/00 , C07D471/06 , C07K14/6555
摘要: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8β-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2
摘要翻译: 公开了一系列在体内保持生长抑素和多巴胺活性的生长抑素 - 多巴胺嵌合类似物。 一个例子是:6-正丙基-8β-麦角酰甲基硫代乙酰基-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH 2
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公开(公告)号:US07109166B1
公开(公告)日:2006-09-19
申请号:US10048856
申请日:2000-08-16
IPC分类号: A61K38/12 , A61K9/52 , A61K9/14 , A61K38/00 , A61K47/30 , A61K47/12 , A61K47/48 , A61K31/74 , A61K9/00 , A61K38/04 , A61K38/31 , A61P1/00 , A61P1/12 , A61P35/02
CPC分类号: A61K47/593 , Y10S514/806 , Y10S514/867 , Y10S514/908 , Y10S514/951 , Y10S514/964
摘要: This invention is directed to a sustained release composition comprised of Compound (A) having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprised of poly-(I)-lactic-glycolic-tartaric acid wherein the amino group of Compound (A) is ionically bound to a carboxyl group of the copolymer and wherein further the composition may be made into a sustained release pharmaceutical composition with pharmaceutically acceptable carrier(s).
摘要翻译: 本发明涉及由具有下式的化合物(A)或其药学上可接受的盐组成的持续释放组合物和由聚(I) - 乳酸 - 乙醇酸 - 酒石酸组成的共聚物,其中化合物(A )与共聚物的羧基离子结合,并且其中该组合物还可以制成具有药学上可接受的载体的缓释药物组合物。
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公开(公告)号:US20050089576A1
公开(公告)日:2005-04-28
申请号:US10990033
申请日:2004-11-16
CPC分类号: A61K47/593 , Y10S514/806 , Y10S514/867 , Y10S514/908 , Y10S514/951 , Y10S514/964
摘要: This invention pertains to a sustained release complex, Compound (I), which comprises Compound (A), having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprising poly-(I)-lactic-glycolic-tartaric acid (P(I)LGT), wherein the amino group of said Compound (A) is ionically bound to a carboxyl group of the P(I)LGT. The present invention further pertains to a process for making said sustained release complex. Further still, the present invention is directed to a pharmaceutical composition comprising said sustained release complex and a pharmaceutically acceptable carrier(s).
摘要翻译: 本发明涉及包含具有下式的化合物(A)或其药学上可接受的盐的包含聚(I) - 乳酸 - 乙醇酸 - 酒石酸(P( I)LGT),其中所述化合物(A)的氨基与P(I)LGT的羧基离子结合。 本发明还涉及制备所述持续释放复合物的方法。 此外,本发明涉及包含所述持续释放复合物和药学上可接受的载体的药物组合物。
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公开(公告)号:US5084555A
公开(公告)日:1992-01-28
申请号:US502438
申请日:1990-03-30
申请人: David H. Coy , Jacques-Pierre Moreau , Sun H. Kim
发明人: David H. Coy , Jacques-Pierre Moreau , Sun H. Kim
IPC分类号: A61K38/00 , A61K38/22 , A61P1/00 , A61P3/08 , A61P35/00 , C07K7/02 , C07K7/06 , C07K7/08 , C07K7/18 , C07K14/575
CPC分类号: C07K14/57572 , C07K7/02 , C07K7/086 , C07K7/18 , A61K38/00
摘要: A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.
摘要翻译: 具有活性位点和负责肽结合的结合位点的生物活性水陆两栖铃蟾肽,哺乳动物胃泌素释放肽(GRP)或哺乳动物生长激素释放因子(GRF)的线性(即非循环)类似物 到目标细胞上的受体。 在天然存在的铃蟾肽,GRP或GRF的活性位点中肽键的切割对于体内生物活性是不必要的。 类似物具有以下修饰之一:(a)活性位点内的氨基酸残基的缺失和活性位点之外的氨基酸残基的修饰,(b)在活性位点内置换两个氨基酸残基 具有合成氨基酸,β-氨基酸或γ-氨基酸残基的位点,或(c)非肽键代替活性位点的氨基酸残基与相邻氨基酸残基之间的肽键 。
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公开(公告)号:US09458195B2
公开(公告)日:2016-10-04
申请号:US13074565
申请日:2011-03-29
IPC分类号: A61K38/00 , C07K7/00 , C07K7/06 , C07K7/08 , C07K14/665
CPC分类号: C07K7/06 , A61K38/00 , C07K7/08 , C07K14/665
摘要: The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.
摘要翻译: 本发明涉及下列化合物:ƒ€ƒ€ƒ€ƒ€ƒ€ƒAc-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp -Cys)-NH 2及其药学上可接受的盐。 该化合物作为一种或多种黑皮质素受体的配体。 本发明还涉及使用该化合物治疗哺乳动物的方法和包含所述化合物的药物组合物。
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公开(公告)号:US07943575B2
公开(公告)日:2011-05-17
申请号:US10506263
申请日:2003-03-04
IPC分类号: A61K38/22
CPC分类号: A61K9/0024 , A61K9/0019 , A61K31/13 , A61K31/4045 , A61K31/428 , A61K31/473 , A61K31/48 , A61K31/4985 , A61K38/23 , A61K38/24 , A61K38/25 , A61K38/29 , A61K47/26 , A61K47/42
摘要: The invention features a method of administering one or more therapeutic agents to a patient and delivering said agent or agents continuously over an extended period of time, said method comprising: obtaining a pharmaceutical composition including a peptide carrier, one or more therapeutic agents, and up to 30 percent, by weight, of a pharmaceutically acceptable, soluble, monomeric carrier; and parenterally administering said pharmaceutical composition to a subject by injection, wherein said composition automatically forms a gel after interaction with the patient's bodily fluids and releases said peptide carrier and said agent or agents continuously within the patient over an extended period.
摘要翻译: 本发明的特征在于向患者施用一种或多种治疗剂并且在延长的时间段内连续递送所述药剂或药剂的方法,所述方法包括:获得药物组合物,其包含肽载体,一种或多种治疗剂和上 至30重量%的药学上可接受的可溶性单体载体; 并通过注射将所述药物组合物肠胃外施用于受试者,其中所述组合物在与患者的体液相互作用后自动形成凝胶,并在长时间内将所述肽载体和所述药剂或药剂在患者体内连续释放。
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公开(公告)号:US20080161233A1
公开(公告)日:2008-07-03
申请号:US11927011
申请日:2007-10-29
CPC分类号: A61K47/593 , Y10S514/806 , Y10S514/867 , Y10S514/908 , Y10S514/951 , Y10S514/964
摘要: This invention pertains to a sustained release complex, Compound (I), which comprises Compound (A), having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprising poly-(I)-lactic-glycolic-tartaric acid (P(I)LGT), wherein the amino group of said Compound (A) is ionically bound to a carboxyl group of the P(I)LGT. The present invention further pertains to a process for making said sustained release complex. Further still, the present invention is directed to a pharmaceutical composition comprising said sustained release complex and a pharmaceutically acceptable carrier(s).
摘要翻译: 本发明涉及包含具有下式的化合物(A)或其药学上可接受的盐的包含聚(I) - 乳酸 - 乙醇酸 - 酒石酸(P( I)LGT),其中所述化合物(A)的氨基与P(I)LGT的羧基离子结合。 本发明还涉及制备所述持续释放复合物的方法。 此外,本发明涉及包含所述持续释放复合物和药学上可接受的载体的药物组合物。
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公开(公告)号:US6150333A
公开(公告)日:2000-11-21
申请号:US361394
申请日:1999-07-26
CPC分类号: A61K38/31
摘要: The present invention is directed to a method of treating one or more of the following disease and/or conditions, which comprises administering to a patient in need thereof the compound H-.beta.-D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH.sub.2, where the Cysteines are bonded by a disulfide bond, or a pharmaceutically acceptable salt thereof, most preferably the acetate salt of the compound, in the treatment of certain diseases and/or conditions such as gastroenterological conditions and/or diseases, endocrinological diseases and/or conditions, various types of cancers and conditions associated with cancer such as cancer cachexia and in the treatment of hypotension and panic attacks.
摘要翻译: 本发明涉及一种治疗以下疾病和/或病症中的一种或多种的方法,其包括向有需要的患者施用化合物H-β-D-Nal-Cys-Tyr-D-Trp-Lys -Val-Cys-Thr-NH2,其中半胱氨酸通过二硫键键合,或其药学上可接受的盐,最优选化合物的乙酸盐,用于治疗某些疾病和/或病症如胃肠病学和 /或疾病,内分泌疾病和/或病症,与癌症如癌症恶病质相关的各种类型的癌症和病症以及治疗低血压和恐慌发作。
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19.
公开(公告)号:US06087337A
公开(公告)日:2000-07-11
申请号:US89410
申请日:1993-07-09
IPC分类号: A61K38/04 , A61K38/00 , A61P35/00 , C07K14/655 , A61K38/16
CPC分类号: C07K14/6555 , A61K38/00 , Y10S514/806
摘要: A method of treating a mammal suffering from benign or malignant proliferative skin disease, e.g., melanoma or malignant skin metastases of melanoma, by topically administering to the mammal at the site of said diseased skin an effective amount of a somatostatin analog containing six or more amino acids.
摘要翻译: 一种治疗患有良性或恶性增殖性皮肤病,例如黑素瘤或黑色素瘤恶性皮肤转移的哺乳动物的方法,其通过在所述患病皮肤部位局部施用有效量的含有六个或更多个氨基的生长抑素类似物 酸。
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公开(公告)号:US6083915A
公开(公告)日:2000-07-04
申请号:US698681
申请日:1991-05-10
IPC分类号: A61K38/00 , A61K38/04 , A61K38/10 , A61K38/22 , A61P1/16 , A61P35/00 , C07K7/06 , C07K7/08 , A61K38/08
CPC分类号: A61K38/105 , Y10S514/894 , Y10S530/828
摘要: A method of treating liver cancer involving administration to the subject a therapeutically effective amount of a bombesin analog.
摘要翻译: 一种治疗肝癌的方法,涉及向受试者施用治疗有效量的铃蟾肽类似物。
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