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1. 发明申请

WO2013095903A1 NOVEL GH-RH ANALOGS WITH POTENT AGONISTIC EFFECTS 审中-公开
标题翻译：新的GH-RH模拟与POTENT激发效应
公开(公告)号：WO2013095903A1
公开(公告)日：2013-06-27
申请号：PCT/US2012/067690
申请日：2012-12-04
申请人： SCHALLY, Andrew, V. , CAI, Ren-Zhi , ZARANDI, Marta , UNIVERSITY OF MIAMI , UNITED STATES OF AMERICA REPRESENTED BY THE DEPARMENT OF VETERANS AFFAIRS
发明人： SCHALLY, Andrew, V. , CAI, Ren-Zhi , ZARANDI, Marta
IPC分类号： C07K14/60 , A61K38/25
CPC分类号： C07K14/60 , A61K38/00 , C07K14/61
摘要： The synthetic peptides have the sequence: [RrA\ A 2 , A 6 , A 8, A 11 , A 12 , A 15 , A 20 , A 21 , A 22 , Nle 27 , A 28 , A 29 , A30]hGH-RH(1 -30)-R 2 (SEQ ID NO: 1 ) wherein R 1 is Ac, Tfa, or is absent, A 1 is Tyr, Dat, or N-Me-Tyr, A 2 is Ala, D-Ala, Abu, or D-Abu, A 6 is Phe or Fpa5, A 8 is Asn, Ala, Gin, Thr, or N-Me-Ala, A 11 is Arg, His, or Har, A 12 is Orn, or Lys(Me)2, A 15 is Abu or Ala A 20 is Arg, His, or Har, A 21 is Orn, or Lys(Me)2, A 22 is Leu, or Orn, A 28 is Ser, or Asp, A 29 is Arg, Har, Agm, D-Arg, or D-Har, A 30 is Arg, Agm, Ada, Amc, Aha, Apa, Har, D-Arg, D-Har, Gab, Gin, D-GIn, Gin-Gab, D-Gln-Gab, or is absent, R 2 is -NH 2 , -OH, -NHR 2 , -N(R 2 ) 2 , or -OR 2 , in which R 2 is any of C 1-12 alkyl, C 2-12 alkenyl, or C 2-12 alkinyl, provided that if A 29 is Agm then A 30 and R 2 are absent A 1 is N-Me-Tyr only, and pharmaceutically acceptable salts thereof.
摘要翻译：合成肽具有以下序列：[RrA / A2，A6，A8，A11，A12，A15，A20，A21，A22，Nle27，A28，A29，A30] hGH-RH（1-30）-R2（SEQ ID NO ：1）其中R1是Ac，Tfa或不存在，A1是Tyr，Dat或N-Me-Tyr，A2是Ala，D-Ala，Abu或D-Abu，A6是Phe或Fpa5，A8是 Asn，Ala，Gin，Thr或N-Me-Ala，A11是Arg，His或Har，A12是Orn或Lys（Me）2，A15是Abu或Ala A20是Arg，His或Har，A21 是Orn或Lys（Me）2，A22是Leu或Orn，A28是Ser或Asp，A29是Arg，Har，Agm，D-Arg或D-Har，A30是Arg，Agm，Ada，Amc ，Aha，Apa，Har，D-Arg，D-Har，Gab，Gin，D-Gln，Gin-Gab，D-Gln-Gab，或不存在，R 2是-NH 2，-OH，-NHR 2，-N （R2）2或-OR2，其中R2是C1-12烷基，C2-12烯基或C2-12炔基中的任何一个，条件是如果A29是Agm，则A30和R2不存在A1是N-Me-Tyr 仅及其药学上可接受的盐。

2. 发明申请

WO2011034976A1 FLUORINATED GHRH ANTAGONISTS 审中-公开
标题翻译：氟化GHRH拮抗剂
公开(公告)号：WO2011034976A1
公开(公告)日：2011-03-24
申请号：PCT/US2010/049008
申请日：2010-09-15
申请人： SCHALLY, Andrew, V. , VARGA, Jozsef, L. , ZARANDI, Marta , CAI, Ren, Zhi , UNIVERSITY OF MIAMI , UNITED STATES OF AMERICA
发明人： SCHALLY, Andrew, V. , VARGA, Jozsef, L. , ZARANDI, Marta , CAI, Ren, Zhi
IPC分类号： C07K14/61 , A61K38/25
CPC分类号： A61K9/0019 , A61K38/00 , C07K14/60
摘要： The present invention relates to novel fluorinated synthetic analogs of hGH-RH(1-3O)NH 2 that inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells, and to therapeutic compositions containing these novel peptides and their use.
摘要翻译：本发明涉及抑制哺乳动物垂体生长激素释放以及抑制人类癌症增殖的hGH-RH（1-3O）NH2的新型氟化合成类似物，并抑制人类癌症的增生和良性增殖性疾病通过直接作用于癌和非恶性细胞的各种器官，以及含有这些新肽的治疗组合物及其用途。

3. 发明申请

WO2005016953A3 ANTAGONISTIC ANALOGS OF GH-RH (2003) 审中-公开
公开(公告)号：WO2005016953A3
公开(公告)日：2005-02-24
申请号：PCT/US2004/024183
申请日：2004-07-26
申请人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND (A NOT FOR PROFIT CORPORATION) , SCHALLY, Andrew, V. , VARGA, Jozsef , ZARANDI, Marta , CAI, Ren, Zhi
发明人： SCHALLY, Andrew, V. , VARGA, Jozsef , ZARANDI, Marta , CAI, Ren, Zhi
IPC分类号： A61K38/00
摘要： There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1-29)NH 2 . These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore prevent the release of growth hormone. The analogs also inhibit the proliferation of human cancers through a direct effect on the cancer cells. The higher inhibitory potencies of the new analogs, as compared to previously described ones, results from replacement of various amino acids.

4. 发明申请

WO1994021674A1 POLYPEPTIDE BOMBESIN ANTAGONISTS 审中-公开
标题翻译：多肽BOMBESIN拮抗剂
公开(公告)号：WO1994021674A1
公开(公告)日：1994-09-29
申请号：PCT/US1994002511
申请日：1994-03-07
申请人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND , SCHALLY, Andrew, V. , CAI, Ren, Zhi
发明人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
IPC分类号： C07K07/08
CPC分类号： C07K7/086 , A61K38/00
摘要： Pseudopeptides comprising a peptide of formula (I): X-A -A -Trp-Ala-Val-Gly-His-Leu-p &cir& _s &cir& _i &cir& _-A -Q wherein X is hydrogen, a single bond linking the alpha amino group of A to the gamma carboxyl moiety on the 3-priopionyl moiety of A when A is Glu, or a group of formula R CO- wherein R is selected from the groups consisting of: a) hydrogen, C1-10alkyl, phenyl or phenyl-C1-10-alkyl, p-Hl-phenyl, p-Hl-phenyl-C1-10-alkyl, naphthyl, naphthyl-C1-10-alkyl, indolyl, indolyl-C1-10-alkyl, pyridyl, pyridyl-C1-10-alkyl, thienyl, thienyl-C1-10-alkyl, cyclohexyl or cyclohexyl-C1-10-alkyl, where Hl = F, Cl, Br, OH, CH3 or OCH3; b) N(R )(R )-, wherein R is hydrogen, C1-10alkyl, phenyl or phenyl-C1-10-alkyl, R is hydrogen or C1-10alkyl; c) R O-, wherein R is C1-10alkyl, phenyl or phenyl-C1-10-alkyl; A is a D- or L-amino acid residue selected from the group consisting of Phe, p-Hl-Phe, pGlu, Nal, Pal, Tpi, unsubstituted Trp or Trp substituted in the benzene ring by one or more members selected from the group consisting of F, Cl, Br, NH2 or C1-3alkyl; or A is a peptide bond linking the acyl moiety of R CO- to the alpha amino moiety of A ; A is Gln, Glu[-], Glu(Y) or His, wherein [-] is a single bond linking the gamma carboxyl group of A when A is Glu with the alpha amino group of A where X is a single bond, Y is -OR or -N(R )(R ) wherein R is hydrogen, C1-3alkyl or phenyl; R is hydrogen or C1-3alkyl; and R is hydrogen, C1-3alkyl or -NHCONH2; Leu-p &cir& _s &cir& _i &cir& _- is a reduced form of Leu wherein the C = O moiety of Leu is instead -CH2- such that the bond of this -CH2- moiety with the alpha amino moiety of the adjacent A residue is a pseudopeptide bond; A is Tac, MTac, or DMTac; and Q is NH2 or OQ where Q is hydrogen, C1-10alkyl, phenyl or phenyl-C1-10-alkyl; and the pharmaceutically acceptable acids or salts thereof.
摘要翻译：包含式（I）的肽的假肽：XA 1 -A 2 -Trp-Ala-Val-Gly-His-Leu-p＆cir＆amp; s＆cir＆amp; A-A 9 -Q其中X是氢当A 2为Glu时，将A 1的α氨基与A 2的3-取代基部分上的γ羧基部分连接的单键，或式R 1 CO-的基团，其中 R 1选自：a）氢，C 1-10烷基，苯基或苯基-C 1-10 - 烷基，对-1-苯基，对-1-苯基-C1-10-烷基，萘基，萘基-C 1-10烷基，吲哚基，吲哚基C 1-10 - 烷基，吡啶基，吡啶基-C 1-10烷基，噻吩基，噻吩基-C1-10-烷基，环己基或环己基-C1-10-烷基，其中H1 = F，Cl，Br，OH，CH 3或OCH 3; b）N（R 2）（R 3） - ，其中R 2是氢，C 1-10烷基，苯基或苯基-C 1-10烷基，R 3是氢或C 1-10烷基; c）R 4 O-，其中R 4是C 1-10烷基，苯基或苯基-C 1-10 - 烷基; A 1是选自由Phe，p-H1-Phe，pGlu，Nal，Pal，Tpi组成的组的D-或L-氨基酸残基，在苯环中被一个或多个成员取代的未取代的Trp或Trp 选自F，Cl，Br，NH 2或C 1-3烷基; 或A 1是将R 1 CO-的酰基部分与A 2的α氨基部分连接的肽键; A 2是Gln，Glu [ - ]，Glu（Y）或His，其中[ - ]是当A 2是Glu时与A 2的γ羧基连接的单键， A 1其中X是单键，Y是-OR 5或-N（R 5）（R 6），其中R 5是氢，C 1-3烷基或苯基; R 6是氢或C 1-3烷基; 和R 7是氢，C 1-3烷基或-NHCONH 2; Leu-p＆cir＆_ s＆cir＆_i＆cir _ _是Leu的还原形式，其中Leu的C = O部分代替-CH2-，使得该-CH 2 - 部分与相邻A <9的α氨基部分的键 >残基是假肽键; A <9>是Tac，MTac或DMTac; Q是NH 2或OQ 1，其中Q 1是氢，C 1-10烷基，苯基或苯基-C 1-10 - 烷基; 和其药学上可接受的酸或其盐。

5. 发明申请

WO2005016953A2 ANTAGONISTIC ANALOGS OF GH-RH (2003) 审中-公开
标题翻译： GH-RH的ANTAGONISTIC ANALOGS（2003）
公开(公告)号：WO2005016953A2
公开(公告)日：2005-02-24
申请号：PCT/US2004024183
申请日：2004-07-26
申请人： UNIV TULANE , SCHALLY ANDREW VICTOR , VARGA JOZSEF , ZARANDI MARTA , CAI REN ZHI
发明人： SCHALLY ANDREW V , VARGA JOZSEF , ZARANDI MARTA , CAI REN ZHI
IPC分类号： A61K38/00 , C07K20060101 , C07K14/60 , C07K
CPC分类号： C07K14/60 , A61K38/00
摘要： There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1-29)NH2. These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore prevent the release of growth hormone. The analogs also inhibit the proliferation of human cancers through a direct effect on the cancer cells. The higher inhibitory potencies of the new analogs, as compared to previously described ones, results from replacement of various amino acids.
摘要翻译：提供了一系列hGH-RH（1-29）NH2的合成拮抗类似物系列。这些类似物抑制内源性hGH-RH对垂体GH-RH受体的活性，因此防止生长激素的释放。类似物还通过对癌细胞的直接作用来抑制人类癌症的增殖。与之前描述的相比，新类似物的更高的抑制效力来自各种氨基酸的替换。

6. 发明申请

WO1992009626A1 NONAPEPTIDE BOMBESIN ANTAGONISTS 审中-公开
标题翻译：非特异性BOMBESIN ANTAGONISTS
公开(公告)号：WO1992009626A1
公开(公告)日：1992-06-11
申请号：PCT/US1991008534
申请日：1991-11-15
申请人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND , SCHALLY, Andrew, V. , CAI, Ren, Zhi
发明人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
IPC分类号： C07K07/02
CPC分类号： C07K7/086 , A61K38/00 , Y02P20/55
摘要： The novel pseudo polypeptides of this invention are potent bombesin antagonists. There are provided processes for their production, pharmaceutical compositions comprising said polypeptides and their use as pharmaceutically active agents. More particularly the present invention provides pseudopeptides comprising a nonapeptide moiety of formula (I): X-A?1-A2-A3-A4-A5-A6-A7-A8¿-psi-A9-Q, wherein Q is NH¿2? or OQ?1¿ where Q1 is hydrogen, C¿1-10?alkyl, phenyl or phenyl-C7-10-alkyl; X is hydrogen or a single bond linking to A?2¿, the acyl residue of an organic acid, or a group of formula R1CO- wherein 1) R1 is hydrogen, C¿1-10?alkyl, phenyl or phenyl-C7-10-alkyl; 2) R?1¿CO- is a) R2.N(R3)-CO- wherein R2 is hydrogen, C¿1-10?alkyl, phenyl or C7-10phenyl-C7-10-alkyl, R?3¿ is hydrogen or C¿1-10? alkyl; b) R?4¿-O-CO- wherein R4 is C¿1-10?alkyl, phenyl or phenyl-C7-10-alkyl. A?1¿ is D-, L- or DL-pGlu, Nal, Phe, Thi, Tyr, Tpi, Hca, Hpp, Mpp, Trp or Trp substituted in the benzene ring by one or more members selected from the group consisting of halogen, NO¿2?, NH2, OH, C1-3 alkyl and C1-3 alkoxy wherein halogen is fluorine, chlorine and bromine, A?2¿ is Asn, Dpa, Gln, His, MeHis, His(Bz), His(Z) or a group of formula Dpa (X), Asp (Y), Glu [-] and Glu (Y); wherein X is as above, Y is -OR?5 or R6-NR7¿ wherein R5 is hydrogen, C¿1-3?alkyl or phenyl; R?6¿ is hydrogen or C¿1-3?alkyl; R?7¿ is hydrogen, C¿1-3?alkyl or -NHCONH2 and [-] is a single bond linking the side carboxyl group with the alpha amino group of A?1¿ where X is a single bond, A3 is Nal, Pal, Tpi, Trp, MeTrp, Trp(For) or Trp substituted in the benzene ring by one or more members selected from the group consisting of halogen, NO¿2?, NH2, OH, C1-3 alkyl and C1-3 alkoxy wherein halogen is fluorine, chlorine and bromine; A?4¿ is Ala, MeAla or Gln; A5 is Val or MeVal; A6 is Gly, Phe or D-Ala; A7 is His, MeHis, His(Bz), His(Z), Lys(Z) or Pal; A8 is a reduced isostere of Leu or Phe; A9 is Leu, Phe, Tpi, Trp or Trp substituted in the benzene ring by one or more members selected from the group consisting of halogen, NO¿2?, NH2, OH, C1-3alkyl and C1-3alkoxy wherein halogen is fluorine, chlorine and bromine; provided that where A?9¿ is Leu or Phe, A1 is other than D-Nal or DL-Phe and where A1 is D-Nal or DL-Phe, A9 is other than Leu or Phe and the salts thereof with pharmaceutically acceptable acids.

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