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公开(公告)号:US08324386B2
公开(公告)日:2012-12-04
申请号:US12587452
申请日:2009-10-07
IPC分类号: C07D457/00
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.
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公开(公告)号:US07579435B2
公开(公告)日:2009-08-25
申请号:US10479771
申请日:2002-06-07
IPC分类号: C07K7/00
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-β-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:US07572883B2
公开(公告)日:2009-08-11
申请号:US11434273
申请日:2006-05-15
IPC分类号: C07K7/00
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
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公开(公告)号:US06180619B2
公开(公告)日:2001-01-30
申请号:US09098393
申请日:1998-06-16
申请人: Sun H. Kim
发明人: Sun H. Kim
IPC分类号: A61K3133
CPC分类号: C07D513/04 , A61K38/00 , C07C323/60 , C07D217/26 , C07D241/04 , C07D285/36 , C07D285/38 , C07D339/00 , C07D417/06 , C07D417/14 , C07D513/14 , C07K5/0606 , C07K5/081
摘要: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.
摘要翻译: 能够抑制异戊烯基转移酶活性的化合物家族。 这些化合物被以下四种化合物所覆盖。在本公开中定义了每个R基团。
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公开(公告)号:US5162497A
公开(公告)日:1992-11-10
申请号:US282328
申请日:1988-12-09
IPC分类号: A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K14/575 , C07K14/685
CPC分类号: C07K7/086 , C07K14/57572 , C07K14/685 , C07K7/02 , C07K7/18 , A61K38/00 , Y10S514/803
摘要: A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.
摘要翻译: 包含9或10个氨基酸残基和至少一个[CH 2 N H]假肽键的缓激肽类似物,该类似物可用作天然存在的缓激肽的拮抗剂或激动剂。
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公开(公告)号:US4814335A
公开(公告)日:1989-03-21
申请号:US66262
申请日:1987-06-23
申请人: Sun H. Kim
发明人: Sun H. Kim
IPC分类号: A61K9/00 , A61K31/505 , A61K31/517 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/00 , C07D239/70 , C07D239/95 , C07D491/048 , C07D495/04 , D06M13/02 , D06M13/322 , D06M13/35 , D06M13/355 , D06M13/402 , D06M23/00 , C07D487/00
CPC分类号: C07D239/95 , C07D239/70
摘要: In one aspect, compounds having antiviral activity and having the general formula: ##STR1## wherein each R.sup.2, independently, is H or lower (fewer than 6 carbon atoms) alkyl; each R.sup.3, independently, is H or lower alkyl; R.sup.0 is H or lower alkyl; R.sup.1 is H or lower alkyl; 1.ltoreq.n.ltoreq.11; n-2.ltoreq.m.ltoreq.2n; 0.ltoreq.p.ltoreq.3; z is 0 or 1; and p.ltoreq.1.ltoreq.2p; each n, m, p, and q being selected so that the sp.sup.3 valence shell of each carbon atom in each ring is filled; or a pharmaceutically acceptable salt thereof.
摘要翻译: 一方面,具有抗病毒活性并具有以下通式的化合物:其中每个R 2独立地为H或更低(少于6个碳原子)烷基; 每个R 3独立地是H或低级烷基; R 0是H或低级烷基; R1是H或低级烷基; 1 = n = 11; n-2 = m 2n; 0 = p = 3; z为0或1; 和p = 1 = 2p; 选择每个n,m,p和q,使得每个环中每个碳原子的sp 3价壳被填充; 或其药学上可接受的盐。
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公开(公告)号:US4598067A
公开(公告)日:1986-07-01
申请号:US661354
申请日:1984-10-16
申请人: Sun H. Kim
发明人: Sun H. Kim
IPC分类号: C07D487/04 , A61K31/415 , A61K31/47 , A61K31/472 , A61K38/00 , A61P1/04 , C07C67/00 , C07C231/00 , C07C237/12 , C07D207/28 , C07D217/16 , C07D217/26 , C07D233/64 , C07D403/12 , C07D471/04 , C07K5/06 , C07K5/078 , A61K37/43 , C07K5/08
CPC分类号: C07D403/12 , C07D207/28 , C07D471/04 , C07K5/06026 , C07K5/06173 , A61K38/00
摘要: A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is N--Ac--Sar, pGlu, or homo-pGlu-; B is an aryl group, a heteroaryl group, a cycloalkyl group, an aralkyl group, a heteroalkyl group, a heteroaralkyl group, a benzoyl group, an alkyl group, an acetyl group, or a substituted aryl group wherein the substituent is halogen, hydroxy, alkoxy, nitro, cyano, or hydroxyalkyl; E is H or an alkyl group; B and E being separate substituents or, together with C.sub.1 and the nitrogen atom to which B is attached, forming a 5,6, or 7-membered ring; m is an integer between 0 and 4; either F is ##STR2## wherein R is an alkoxy group or an aralkoxy group; or F is ##STR3## and is capable of forming a 6-membered ring with the nitrogen atom of A, provided that F can only be ##STR4## forming a ring with A when A is pGlu or homo-pGlu.
摘要翻译: 具有式“IMAGE”的化合物或其药学上可接受的盐,其中A是N-Ac-Sar,pGlu或homo-pGlu-; B是芳基,杂芳基,环烷基,芳烷基,杂烷基,杂芳烷基,苯甲酰基,烷基,乙酰基或取代的芳基,其中取代基是卤素,羟基 ,烷氧基,硝基,氰基或羟基烷基; E是H或烷基; B和E是独立的取代基,或者与C1和与B连接的氮原子一起形成5,6或7-元环; m是0和4之间的整数; F是F,其中R是烷氧基或芳烷氧基; 或者F是
,并且能够与A的氮原子形成6元环,条件是当A是pGlu或homo-pGlu时,F只能与A形成环。 -
公开(公告)号:US4495193A
公开(公告)日:1985-01-22
申请号:US454733
申请日:1982-12-30
申请人: Sun H. Kim , Jacques-Pierre Moreau
发明人: Sun H. Kim , Jacques-Pierre Moreau
IPC分类号: C07D209/46 , C07D403/06 , C07D403/12 , A61K31/415
CPC分类号: C07D403/06 , C07D209/46 , C07D403/12
摘要: A compound having gastric acid secretion reducing activity and having the formula ##STR1## wherein each V and W, independently, is H, --CH.sub.2 COOR.sup.4 where R.sup.4 is H or lower alkyl, --CH.sub.2 CN, or ##STR2## or V and W together represent .dbd.CHCOOR.sup.4 or .dbd.CHCN; A is ##STR3## R.sup.1 is H or CH.sub.3 ; L is CH.sub.2 S; Q is O or CH.sub.2 S; n is 0 or 1; 2 m 4; each R.sup.2 and R.sup.3, independently, is hydrogen, lower alkyl, lower cycloalkyl, or lower aralkyl; or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4, 5, or 6 membered heterocyclic ring containing 0, 1, or 2 oxygen atoms and 1, 2, or 3 nitrogen atoms and being unsubstituted or lower alkyl substituted; and Ar is a single ring aromatic group selected from aryl, substituted aryl, fused aryl, or heteroaryl; or the pharmaceutically acceptable salt thereof.
摘要翻译: 具有胃酸分泌降低活性并具有下式的化合物:其中每个V和W独立地是H,-CH 2 COOR 4,其中R 4是H或低级烷基,-CH 2 CN或V和W一起代表= CHCOOR4或= CHCN; A是
+ TR R1是H或CH3; L是CH2S; Q是O或CH2S; n为0或1; 2 m 4; 每个R 2和R 3独立地是氢,低级烷基,低级环烷基或低级芳烷基; 或R 2和R 3与它们所连接的氮原子一起形成含有0,1或2个氧原子和1,2或3个氮原子的4,5或6元杂环,并且是未取代的或低级的 烷基取代; Ar为选自芳基,取代芳基,稠合芳基或杂芳基的单环芳基; 或其药学上可接受的盐。 -
公开(公告)号:US08178651B2
公开(公告)日:2012-05-15
申请号:US12456715
申请日:2009-06-22
IPC分类号: C07K7/00
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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