-
公开(公告)号：US5493006A
公开(公告)日：1996-02-20
申请号：US078558
申请日：1993-06-16
IPC分类号： A61K38/00 , C07K14/575 , C07K14/695
CPC分类号： C07K14/57509 , A61K38/00
摘要： Improved CRF peptide antagonists have the formula: ##STR1## wherein R.sub.20 is Cys or Glu; R.sub.23 is Cys, Lys or Orn; provided that when R.sub.20 is Cys, R.sub.23 is Cys and when R.sub.20 is Glu, R.sub.23 is Lys or Orn; or a nontoxic addition salt thereof. Specific CRF antagonists disclosed include (cyclo 20-23) [D-Phe.sup.12, Lys.sup.23, Nle.sup.21,38, ]rCRF(12-41); (cyclo 20-23) [D-Phe.sup.12, Orn.sup.23, Nle.sup.21,38 ]rCRF(12-41) and (cyclo 20-23) [D-Phe.sup.12, Cys.sup.20, Cys.sup.23, Nle.sup.21,38 ]rCRF(12-41).
摘要翻译： 改进的CRF肽拮抗剂具有下式：其中R 20是Cys或Glu; R23是Cys，Lys或Orn; 条件是当R 20为Cys时，R 23为Cys，当R 20为Glu时，R 23为Lys或Orn; 或其无毒的加成盐。 公开的具体CRF拮抗剂包括（环20-23）[D-Phe12，Lys23，Nle21,38] rCRF（12-41）; （环20-23）[D-Phe12，Orn23，Nle21,38] rCRF（12-41）和（环20-23）[D-Phe12，Cys20，Cys23，Nle21,38] rCRF（12-41）。
-
公开(公告)号：US5296468A
公开(公告)日：1994-03-22
申请号：US6729
申请日：1993-01-21
申请人： Carl A. Hoeger , Jean E. F. Rivier , Paula G. Theobald , John S. Porter , Catherine L. Rivier , Wylie W. Vale, Jr.
发明人： Carl A. Hoeger , Jean E. F. Rivier , Paula G. Theobald , John S. Porter , Catherine L. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07C279/24 , C07C279/28 , C07C313/30 , C07D249/14 , C07K7/02 , C07K7/23 , A61K37/38 , C07K7/06 , C07K7/20
CPC分类号： C07K7/02 , C07C279/24 , C07C279/28 , C07C313/30 , C07D249/14 , C07K7/23 , A61K38/00 , C07C2101/14 , Y10S514/80 , Y10S930/11
摘要： Peptides which include unnatural amino acids and which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The antagonists may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions. Such unnatural amino acids are useful in the synthesis of peptides and have the formula U.sup.* : ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; and j=1, 2 or 3. Preferably, either Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pridyl or ##STR3## where R.sub.11 is H or acyl.
摘要翻译： 包括非天然氨基酸的肽，其通过垂体抑制或促进促性腺激素的分泌并抑制性腺释放类固醇。 施用有效量的这种肽作为GnRH拮抗剂可防止雌性哺乳动物卵的排卵和/或由性腺释放类固醇。 拮抗剂可用于治疗类固醇依赖性肿瘤，例如前列腺和乳腺肿瘤。 肽是十肽GnRH的类似物，其中在3-，5-，6-和/或8-位存在至少一个非天然氨基酸残基。 这样的非天然氨基酸可用于肽的合成，并具有其中W是（CH 2）n或（*化学结构*）n是1至6的整数的式U *：（*化学结构*）; 优选地，Y是N-CN，X是NH，R 2是烷基，改性烷基，链烯基，炔基，芳基或甲基酰基或（*化学结构*），其中R 11是H或酰基 。
-
公开(公告)号：US5262519A
公开(公告)日：1993-11-16
申请号：US701414
申请日：1991-05-15
CPC分类号： C07K14/60
摘要： The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans and also resist enzymatic degradation in the body. Certain preferred peptides have the formula:(B)R.sub.1 -Ala-Asp-Ala-Ile-Phe-Thr-R.sub.8 -Ser-Tyr-Arg-Lys-Val-Leu-R.sub.15 -R.sub.16 - Leu-Ser-Ala-Arg-Lys-Leu-Leu-R.sub.24 -R.sub.25 -Ile-Nle-R.sub.28 -Arg-Y wherein R.sub.1 is Tyr, D-Tyr, Phe, D-Phe, His or D-His; B is H or N.sup..alpha. Me; R.sub.8 is Ala, Aib or Asn; R.sub.15 is Gly or Ala; R.sub.16 is Ala, Aib or Gln; R.sub.24 is Ala, Aib or Gln; R.sub.25 is Ala, Aib or Asp; R.sub.28 is Ser or Asn; Y is NHR with R being H or lower alkyl; provided that at least one of R.sub.8, R.sub.16, R.sub.24 and R.sub.25 is Ala or Aib.
-
公开(公告)号：US5245009A
公开(公告)日：1993-09-14
申请号：US715752
申请日：1991-06-14
申请人： Wayne D. Kornreich , Jean-Francois Hernandez , Jean E. F. Rivier , Catherine L. Rivier , Wylie W. Vale, Jr.
发明人： Wayne D. Kornreich , Jean-Francois Hernandez , Jean E. F. Rivier , Catherine L. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57509 , A61K38/00 , Y10S930/26
摘要： Disclosed are improved CRF peptide antagonists such as those having the formula: Y-D-Phe-R.sub.13 -Leu-Leu-Arg-R.sub.17 -R.sub.18 -Leu-R.sub.20 -Nle-R.sub.22 -R.sub.23 -R.sub.24 -R.sub.25 -R.sub.26 -Leu-R.sub.28 -R.sub.29 -Gln-R.sub.31 -R.sub.32 -R.sub.33 -R.sub.34 -Arg-R.sub.36 -R.sub.37 -Nle-R.sub.39 -R.sub.40 -R.sub.41 -NH.sub.2 wherein Y is Ac or hydrogen; R.sub.13 is His, Tyr or Glu; R.sub.17 is Cys, Glu, Asn or Lys; R.sub.18 is Val, Nle or Met; R.sub.20 is D-Cys, Glu, D-Glu, Aib or D-Ala; R.sub.22 is Ala, Aib, Thr, Asp or Glu; R.sub.23 is Arg, Orn, Har or Lys; R.sub.24 is Ala or Aib; R.sub.25 is Asp or Glu; R.sub.26 is Gln, Asn or Lys; R.sub.28 is Ala or Aib; R.sub.29 is Gln, Aib or Glu, R.sub.31 is Ala or Aib; R.sub.32 is His, Aib, Gly, Tyr or Ala; R.sub.33 is Ser, Aib, Asn, Leu, Thr or Ala; R.sub.34 is Asn or Aib; R.sub.36 is Lys, Orn, Arg, Har or Leu; R.sub.37 is Leu or Try; R.sub.39 is Glu, Aib or Asp; R.sub.40 is Ile, Aib, Thr, Glu, Ala, Val, Leu, Nle, Phe, Nva, Gly or Gln; and R.sub.41 is Ala, Ile, Gly, Val, Leu, Nle, Phe, Nva or Gln. Specific CRF antagonists disclosed include [D-Phe.sup.12, D-Ala.sup.20, Nle.sup.21,38,]-rCRF(12-41), [D-Phe.sup.12, Nle.sup.21,38, Aib.sup.33 ]-rCRF(12-41) and (c 17-20) [D-Phe.sup.12, Cys.sup.17, D-Cys.sup.20, Nle.sup.21,38 ]-rCRF(12-41).
摘要翻译： 公开了改进的CRF肽拮抗剂，例如具有下式的那些：肽，如YD-Phe-R13-Leu-Leu-Arg-R17-R18-Leu-R20-Nle-R22-R23-R24-R25-R26-Leu-R2 8- R29-Gln-R31-R32-R33-R34-Arg-R36-R37-Nle-R39-R40-R41-NH2，其中Y是Ac或氢; R13是His，Tyr或Glu; R17是Cys，Glu，Asn或Lys; R18为Val，Nle或Met; R20是D-Cys，Glu，D-Glu，Aib或D-Ala; R22是Ala，Aib，Thr，Asp或Glu; R23是Arg，Orn，Har或Lys; R24是Ala或Aib; R25为Asp或Glu; R26是Gln，Asn或Lys; R28是Ala或Aib; R29是Gln，Aib或Glu，R31是Ala或Aib; R32是His，Aib，Gly，Tyr或Ala; R33是Ser，Aib，Asn，Leu，Thr或Ala; R34是Asn或Aib; R36是Lys，Orn，Arg，Har或Leu; R37是Leu或Try; R39是Glu，Aib或Asp; R40是Ile，Aib，Thr，Glu，Ala，Val，Leu，Nle，Phe，Nva，Gly或Gln; R41是Ala，Ile，Gly，Val，Leu，Nle，Phe，Nva或Gln。 公开的具体的CRF拮抗剂包括[D-Phe12，D-Ala20，Nle21,38] -rCRF（12-41），[D-Phe12，Nle21,38，Aib33] -rCRF（12-41）和（c17- 20）[D-Phe12，Cys17，D-Cys20，Nle21,38] -rCRF（12-41）。
-
公开(公告)号：US5235036A
公开(公告)日：1993-08-10
申请号：US709091
申请日：1991-05-31
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57509 , A61K38/00 , Y10S930/26
摘要： Analogs of CRF, which are based upon hCRF, oCRF and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels. Analogs include those having the formula: Y-R.sub.1 -R.sub.2 -R.sub.3 -R.sub.4 -R.sub.5 -Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-R.sub.20 -R.sub.21 -R.sub.22 -R.sub.23 -R.sub.24 -R.sub.25 -Gln-Leu-Ala-Gln-Gln-Ala-R.sub.32 -Ser-Asn-Arg-Lys-Leu-R.sub.38 -R.sub.39 -Ile-R.sub.41 -NH.sub.2, wherein Y is an acyl group having 7 or fewer carbon atoms or hydrogen; R.sub.1 is Ser or desR.sub.1 ; R.sub.2 is Glu, Gln or desR.sub.2 ; R.sub.3 is Glu or desR.sub.3 ; R.sub.4 is Pro or desR.sub.4 ; R.sub.5 is Pro or desR.sub.5 ; R.sub.20 is Ala or Glu; R.sub.21 is Met or Nle; R.sub.22 is Ala or Thr; R.sub.23 is Arg or Lys; R.sub.24 is D-Ala or Ala; R.sub.25 is Glu or Asp; R.sub.32 is D-His or His; R.sub.38 is Met, Nle or Leu; R.sub.39 is Ala, Glu or Asp; R.sub.41 is Ile or Ala; provided however that at least one of R.sub.20 and R.sub.39 is Ala. One example is [Ala.sup.20 ]-oCRF. These analogs or their pharmaceutically acceptable salts, dispersed in an acceptable liquid or solid carrier, can be administered to humans.
-
公开(公告)号：US5098995A
公开(公告)日：1992-03-24
申请号：US342751
申请日：1989-04-25
IPC分类号： A61K38/04 , A61K38/00 , A61P5/00 , C07K14/575 , C07K14/60
摘要： The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans and also resist enzymatic degradation in the body. The peptides have the sequence: (B)R.sub.1 -R.sub.2 -R.sub.3 -Ala-(Q.sub.1)R.sub.5 -Phe-Thr-R.sub.8 -Ser(Q.sub.2)R.sub.10 -Arg-R.sub.12 -(Q.sub.3)R.sub.13 -Leu-R.sub.15 -Gln-(Q.sub.4)Leu-R.sub.18 -(Q.sub.5)Ala-Arg-R.sub.21 -(Q.sub.6)R.sub.22 -(Q.sub.7)Leu-R.sub.24 -R.sub.25 -(Q.sub.8)R.sub.26 -(Q.sub.9)R.sub.27 -R.sub.28 -Arg-Gln-Gln-Gly-Glu-R.sub.34 -Asn-Gln-Glu-R.sub.38 -R.sub.39 -R.sub.40 -Arg-R.sub.42 -R.sub.43 -R.sub.44 wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His; B is H, C.sup.a Me, N.sup.a Me, desamino, Ac or For; R.sub.2 is Ala, D-Ala, NMA or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.5 is Ile or Leu; R.sub.8 is Ser, Asn, Lys, Arg, Asp or Glu; R.sub.10 is Tyr, D-Tyr or Phe; R.sub.12 is Arg or Lys; R.sub.13 is Ile, Val, Leu or Ala; R.sub.15 is Gly or Ala; R.sub.18 is Ser or Tyr; R.sub.21 is Lys, D-Lys, Arg or D-Arg; R.sub.22 is Leu, Ile, Ala or Val; R.sub.24 is Gln or His; R.sub.25 is Asp or Glu; R.sub.26 is Ile or Leu; R.sub.27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.34 is Ser or Arg; R.sub.38 is Arg or Gln; R.sub.39 is Gly or Arg; R.sub.40 is Ala or Ser; R.sub.42 is Phe, Ala or Val; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid; Q.sub.1 -Q.sub.9 are either H or C.sup.a Me, provided however that one of Q.sub.1 -Q.sub.9 is C.sup.a Me. These peptides may also be used diagnostically, and the C-terminus can be shortened to residue-29.
摘要翻译： 本发明提供了合成肽，其在刺激包括人在内的动物中垂体GH的释放方面非常有效，并且还抵抗体内的酶降解。 肽具有以下顺序：（B）R1-R2-R3-Ala-（Q1）R5-Phe-Thr-R8-Ser（Q2）R10-Arg-R12-（Q3）R13-Leu-R15-Gn- （Q4）Leu-R18-（Q5）Ala-Arg-R21-（Q6）R22-（Q7）Leu-R24-R25-（Q8）R26-（Q9）R27-R28-Arg-Gln-Gln-Gly- Glu-R34-Asn-Gln-Glu-R38-R39-R40-Arg-R42-R43-R44其中R1是Tyr，D-Tyr，Met，Phe，D-Phe，pCl-Phe，Leu，His或D- 他的 B是H，CaMe，NaMe，desamino，Ac或For; R2是Ala，D-Ala，NMA或D-NMA; R3是Asp或D-Asp; R5是Ile或Leu; R8是Ser，Asn，Lys，Arg，Asp或Glu; R10是Tyr，D-Tyr或Phe; R12是Arg或Lys; R13是Ile，Val，Leu或Ala; R15是Gly或Ala; R18为Ser或Tyr; R21为Lys，D-Lys，Arg或D-Arg; R22是Leu，Ile，Ala或Val; R24是Gln或His; R25为Asp或Glu; R26是Ile或Leu; R27是Met，D-Met，Ala，Nle，Ile，Leu，Nva或Val; R28为Asn或Ser; R34是Ser或Arg; R38是Arg或Gln; R39为Gly或Arg; R40是Ala或Ser; R42是Phe，Ala或Val; R43是Asn或Arg; R44是天然氨基酸; Q1-Q9是H或CaMe，但Q1-Q9中的一个是CaMe。 这些肽也可以在诊断上使用，并且C末端可以缩短为残基29。
-
公开(公告)号：US4740500A
公开(公告)日：1988-04-26
申请号：US946454
申请日：1986-12-23
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure: Ac-.beta.-D-NAL-R.sub.2 -D-3PAL-Ser-Arg-R.sub.6 -Leu-Arg-Pro-R.sub.10 wherein R.sub.2 is Cl-D-Phe, F-D-Phe, NO.sub.2 -D-Phe, Br-D-Phe, 3,4Cl.sub.2 -D-Phe or C.alpha.Me-Cl-D-Phe; R.sub.6 is D-3PAL, D-Trp, For-D-Trp, NO.sub.2 -D-Trp, (imBzl)D-His, D-Tyr or .beta.-D-NAL; and R.sub.10 is Gly-NH.sub.2, NHCH.sub.2 CH.sub.3, NHNHCONH.sub.2 or D-Ala-NH.sub.2.
摘要翻译： 抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。 施用有效量防止雌性哺乳动物卵的排卵和/或性腺释放类固醇。 肽具有以下结构：Ac-β-D-NAL-R2-D-3PAL-Ser-Arg-R6-Leu-Arg-Pro-R10，其中R2是Cl-D-Phe，FD-Phe， Phe，Br-D-Phe，3,4Cl2-D-Phe或CαMe-Cl-D-Phe; R6是D-3PAL，D-Trp，For-D-Trp，NO2-D-Trp，（imBz1）D-His，D-Tyr或β-D-NAL; 并且R 10是Gly-NH 2，NHCH 2 CH 3，NHNHCONH 2或D-Ala-NH 2。
-
公开(公告)号：US4652550A
公开(公告)日：1987-03-24
申请号：US653867
申请日：1984-09-21
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure: X-R.sub.1 -R.sub.2 -R.sub.3 -Ser-Tyr-R.sub.6 -R.sub.7 -Arg-Pro-R.sub.10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro or .beta.-D-NAL; R.sub.2 is Cl-D-Phe, F-D-Phe, NO.sub.2 -D-Phe, C.sup..alpha. Me-4-Cl-D-Phe, Cl.sub.2 -D-Phe or Br-D-Phe; R.sub.3 is D-Trp, substituted D-Trp, .beta.-D-NAL, or D-PAL; R.sub.6 is a D-isomer of a lipophilic amino acid or is 4-NH.sub.2 -D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL or D-Arg; R.sub.7 is Nle, Phe, Met, Tyr, Nva, Trp, Cys, PAL or 4F-D-Phe; and R.sub.10 is Gly-NH.sub.2 or D-Ala-NH.sub.2 ; provided however that when R.sub.1 is .beta.-D-NAL, then R.sub.6 is 4-NH.sub.2 -D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL or D-Arg.
摘要翻译： 抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。 施用有效量防止雌性哺乳动物卵的排卵和/或性腺释放类固醇。 肽具有以下结构：X-R1-R2-R3-Ser-Tyr-R6-R7-Arg-Pro-R10，其中X是氢或具有7个或更少碳原子的酰基; R1是脱氢-Pro或β-D-NAL; R2是Cl-D-Phe，F-D-Phe，NO2-D-Phe，CαMe-4-Cl-D-Phe，Cl2-D-Phe或Br-D-Phe; R3是D-Trp，取代的D-Trp，β-D-NAL或D-PAL; R6是亲脂性氨基酸的D-异构体，或者是4-NH2-D-Phe，D-Lys，D-Orn，D-Har，D-His，4-胍-D-Phe，D-PAL或D g R7是Nle，Phe，Met，Tyr，Nva，Trp，Cys，PAL或4F-D-Phe; 而R10为Gly-NH2或D-Ala-NH2; 但是当R1为β-D-NAL时，R6为4-NH2-D-Phe，D-Lys，D-Orn，D-Har，D-His，4-gua-D-Phe，D-PAL 或D-Arg。
-
公开(公告)号：US4565804A
公开(公告)日：1986-01-21
申请号：US648637
申请日：1984-09-07
CPC分类号： C07K7/23 , A61K38/00 , Y10S930/13
摘要： Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure: X-R.sub.1 -(W)D-Phe-R.sub.3 -R.sub.4 -R.sub.5 -R.sub.6 (V)-R.sub.7 -Arg-Pro-R.sub.10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro, Pro, D-pGlu, D-Phe, D-Trp or .beta.-D-NAL; W is F, Cl, Cl.sub.2 Br, NO.sub.2 or C.sup..alpha. Me-Cl; R.sub.3 is D-Trp, (N.sup.in For)D-Trp or D-Trp which is substituted in the 5- or 6-position with NO.sub.2, NH.sub.2, OCH.sub.3, F, Cl, Br or CH.sub.3 ; R.sub.4 is Ser, Orn, AAL or aBu; R.sub.5 is Tyr, (3F)Phe, (2F)Phe, (3I)Tyr, (3CH.sub.3)Phe, (2CH.sub.3)Phe, (3Cl)Phe or (2Cl)Phe; R.sub.6 is D-Lys, D-Orn or D-Dap; V is (arg-R',R").sub.n (X), with n being 1 to 5 and R' and R" being H, methyl, ethyl, propyl or butyl; R.sub.7 is Leu, NML, Nle or Nva; and R.sub.10 is Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR1## where Q is H or lower alkyl.
摘要翻译： 抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。 施用有效量防止雌性哺乳动物卵的排卵和/或性腺释放类固醇。 肽具有以下结构：X-R1-（W）D-Phe-R3-R4-R5-R6（V）-R7-Arg-Pro-R10其中X是氢或具有7个或更少碳原子的酰基; R1是脱氢-Pro，Pro，D-pGlu，D-Phe，D-Trp或β-D-NAL; W是F，Cl，Cl 2 Br，NO 2或CαMe-Cl; R3是在5或6位被NO 2，NH 2，OCH 3，F，Cl，Br或CH 3取代的D-Trp，（NinFor）D-Trp或D-Trp; R4是Ser，Orn，AAL或aBu; R5是Tyr，（3F）Phe，（2F）Phe，（3I）Tyr，（3CH3）Phe，（2CH3）Phe，（3Cl）Phe或（2Cl）Phe; R6是D-Lys，D-Orn或D-Dap; V是（arg-R'，R“'）n（X），n为1至5，R'和R”为H，甲基，乙基，丙基或丁基; R7是Leu，NML，Nle或Nva; 并且R 10是Gly-NH 2，D-Ala-NH 2或NH-Y，其中Y是低级烷基，环烷基，氟低级烷基或者其中Q是H或低级烷基。
-
公开(公告)号：US07851588B2
公开(公告)日：2010-12-14
申请号：US12366816
申请日：2009-02-06
IPC分类号： A61K38/12
CPC分类号： C07K14/47 , A61K38/00 , C07K14/57509
摘要： CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. Some of these analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is:(cyclo 31-34)[Ac-Pro4,D-Phe12,Nle18,21,Glu31,Lys34]-sucker urotensin(4-41).
摘要翻译： 结合CRFR1的CRF肽类似物的亲和力远远大于它们与CRFR2结合的亲和力。 这些类似物中的一些表现出CRF激动剂活性。 可以通过固相合成制备的一个示例性类似物是：（环31-34）[Ac-Pro4，D-Phe12，Nle18,21，Glu31，Lys34]刺激性尿素转运蛋白（4-41）。
-
-
-
-
-
-
-
-
-
搜索结果
117 条记录 (耗时 0.035 秒)
