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1. 发明申请

WO9932510A9 KAPPA RECEPTOR OPIOID PEPTIDES 审中-公开
标题翻译： KAPPA受体OPIOID PEPTIDES
公开(公告)号：WO9932510A9
公开(公告)日：1999-09-23
申请号：PCT/US9827282
申请日：1998-12-22
申请人： FERRING BV , JUNIEN JEAN LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER SUEIRAS , TROJNAR JERZY A , VANDERAH TODD W
发明人： JUNIEN JEAN LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER SUEIRAS , TROJNAR JERZY A , VANDERAH TODD W
IPC分类号： A61K38/00 , A61K38/07 , A61P1/04 , A61P13/00 , A61P13/10 , A61P25/04 , C07K5/10 , C07K5/107 , C07K5/117
CPC分类号： C07K5/1027 , A61K38/00 , C07K5/1016 , C07K5/1024
摘要： Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono- or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED50 of not greater than about 0.5 mg/kg, include H-D-Phe-D-Phe-D-Nle-D-Arg-NHEt, H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr, H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NEt2, H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe, H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl, H-D-4Fpa-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl, H-D-Ala-(2Thi)-D-3, 4Cpa-D-Leu-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Gmf-morpholinyl, H-D-Phe-D-Phe-D-Leu-D-Orn-NH(Aeb), H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl, and H-D-Phe-D-Phe-D-Nle-D-Arg-NH(Hoh).
摘要翻译：产生对κ阿片样物质受体（KOR）具有高选择性且长时间持续的外周作用但不明显进入脑的肽是具有C末端的四个D-异构体氨基酸残基的序列，其是单或二取代酰胺。对KOR具有至少1,000次对μ阿片受体的亲和力和不大于约0.5mg / kg的ED 50的亲和力的代表性化合物包括HD-Phe-D-Phe-D-Nle-D-Arg -NHEt，HD-Phe-D-Phe-D-Nle-D-Arg-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基，HD-Phe-D-Phe -D-Nle-D-Arg-NHPr，HD-Phe-D-Phe-D-Nle-D-Arg-硫代吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NEt2，HD-Phe -D-Phe-D-Nle-D-Arg-NHMe，HD-Phe-D-Phe-D-Leu-D-Orn-吗啉基，HD-4Fpa-D-Phe-D-Nle-D-Arg-NH 4-吡啶甲基，HD-Phe-D-Phe-D-Nle-D-Arg-NH-环丙基，HD-Ala-（2Thi）-D-3,4cpa-D-Leu-D-Arg-吗啉基，HD -Phe-D-Phe-D-Nle-D-Gmf-吗啉基，HD-Phe-D-Phe-D-Leu-D-Orn-NH（Aeb），HD-Phe-D-Phe-D-Leu- D-Lys-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-哌嗪基和HD-Phe-D-Phe-D-Nle-D-Arg-NH（Hoh）。

2. 发明申请

WO2007139921A3 N-OXIDES OF KAPPA OPIOID RECEPTOR PEPTIDES 审中-公开
标题翻译： KAPPA阿片受体肽的N-氧化物
公开(公告)号：WO2007139921A3
公开(公告)日：2008-01-24
申请号：PCT/US2007012463
申请日：2007-05-25
申请人： CARA THERAPEUTICS INC , JUNIEN JEAN-LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER S , TROJNAR JERZY A , VANDERAH TODD W , LEWIS MICHAEL E
发明人： JUNIEN JEAN-LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER S , TROJNAR JERZY A , VANDERAH TODD W , LEWIS MICHAEL E
IPC分类号： C07K5/10 , A61K38/07 , A61P1/00 , A61P13/10 , A61P17/04 , A61P29/00 , A61P37/00 , C07K5/107 , C07K5/117
CPC分类号： C07K5/1016 , A61K38/00
摘要： Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4- picolyl-N-oxide. A preferred compound, which has an affinity for the KOR at least 1,000 times its affinity for the mu opioid receptor and an IC50 for CYP3 A4 of greater than about 10 micromolar, is H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide
摘要翻译：对于κ阿片样物质受体（KOR）与μ-阿片样物质受体显示出高选择性的某些肽，并且很少或没有CYP3A4抑制活性，包括具有C-末端的四个D-异构体氨基酸残基的四肽，其是N-氧化物取代的酰胺如HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基-N-氧化物。 HD-Phe-D-Phe-D-Nle-D-D对于KOR具有对μ-阿片样物质受体的亲和力至少1000倍的亲和力以及大于约10微摩尔的CYP3A4的IC 50的优选化合物，精氨酸-NH-4-吡啶甲基-N-氧化物

3. 发明申请

WO1995002609A1 PEPTIDES EXHIBITING OXYTOCIN ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：肽展示氧化物拮抗活性
公开(公告)号：WO1995002609A1
公开(公告)日：1995-01-26
申请号：PCT/SE1994000674
申请日：1994-07-07
申请人： FERRING B.V. , AURELL, Carl-Johan , MELIN, Per , NILSSON, Anders , TROJNAR, Jerzy
发明人： FERRING B.V.
IPC分类号： C07K07/16
CPC分类号： C07K7/16 , A61K38/00
摘要： A peptide having formula (I) wherein Mpa is 3-mercaptopropionic acid residue (-S-CH2-CH2-CO-); X is D-tryptophan (D-Trp) or beta -(2-Naphtyl)-D-alanine (D-Nal); Ile is isoleucine; Y is alloisoleucine (alloIle) or (S)-2-Amino-3-ethyl-pentanoic acid (Ala( beta -Et2)); Asn is asparagine; alpha -Abu is alpha -aminobutyric acid residue (II) and N alpha MeOrn is N alpha -methyl-ornithine, is disclosed. The peptides may be used as an active ingredient in a medicament, especially in a pharmaceutical composition for therapeutic treatment of excessive uterus muscle contractions.
摘要翻译：具有式（I）的肽，其中Mpa是3-巯基丙酸残基（-S-CH 2 -CH 2 -CO-）; X是D-色氨酸（D-Trp）或β-（2-萘基）-D-丙氨酸（D-Nal）; Ile是异亮氨酸; Y是异亮氨酸（allolle）或（S）-2-氨基-3-乙基 - 戊酸（Ala（β-Et2））; Asn是天冬酰胺 α-Abu是α-氨基丁酸残基（II），NαMeOr是Nα-甲基 - 鸟氨酸。肽可以用作药物，特别是用于治疗性治疗过度子宫肌肉收缩的药物组合物中的活性成分。

4. 发明申请

WO1991013092A1 VASOACTIVE VASOTOCIN DERIVATIVES 审中-公开
标题翻译： VASOACTIVE VASOTOCIN DORIVATIVES
公开(公告)号：WO1991013092A1
公开(公告)日：1991-09-05
申请号：PCT/SE1991000154
申请日：1991-02-26
申请人： FERRING AB , AURELL, Carl-Johan , MELIN, Per , NILSSON, Anders , TROJNAR, Jerzy
发明人： FERRING AB
IPC分类号： C07K07/16
CPC分类号： C07K7/16 , A61K38/00
摘要： Vasotocin derivatives of formula (I), wherein Hmp = a 2-hydroxy-3-mercaptopropionic acid residue (a), Z = Phe or Tyr, Y = Hgn or Hci, X = (b), Q = H or from 1 to 3 amino acid residues of the same or different natural or unnatural L- or D-amino acids, and n is 1, 2 or 3, are disclosed. A pharmaceutical composition which comprises at least one vasotocin derivative as defined above is intended for use as a vasoconstrictive agent.
摘要翻译：式（I）的血管生成物衍生物，其中Hmp = 2-羟基-3-巯基丙酸残基（a），Z = Phe或Tyr，Y = Hgn或Hci，X =（b），Q = H或从1至相同或不同的天然或非天然的L-或D-氨基酸的3个氨基酸残基，n为1,2或3。包含至少一种如上定义的血管生成衍生物的药物组合物意在用作血管收缩剂。

5. 发明申请

WO1989003393A1 VASOACTIVE PEPTIDES 审中-公开
公开(公告)号：WO1989003393A1
公开(公告)日：1989-04-20
申请号：PCT/SE1988000509
申请日：1988-10-04
申请人： FERRING AB , MELIN, Per , TROJNAR, Jerzy
发明人： FERRING AB
IPC分类号： C07K07/16
CPC分类号： C07K7/16 , A61K38/00
摘要： A vasotocin derivative of formula (I) where Hmp is a 2-hydroxy-3-mercaptopropionic acid residue, X is formula (II), Q1 and Q2 are the same or different and are H or from 1 to 3 peptide residues of the same or different natural or unnatural L- or D-amino acids, and n is 1, 2 or 3. A pharmaceutical composition is also described which is intended for use as a vasoconstrictive agent comprising at least one vasotocin derivative as defined above.
摘要翻译：其中Hmp是2-羟基-3-巯基丙酸残基的式（I）的血管生成物衍生物，X是式（II），Q1和Q2相同或不同，是H或相同的1至3个肽残基或不同的天然或非天然的L-或D-氨基酸，n是1,2或3.还描述了一种药物组合物，其用作含有至少一种上述定义的血管生成物衍生物的血管吸收剂。

6. 发明申请

WO1995000548A1 BIOLOGICALLY ACTIVE VASOPRESSIN ANALOGUES 审中-公开
标题翻译：生物活性血管生成素类似物
公开(公告)号：WO1995000548A1
公开(公告)日：1995-01-05
申请号：PCT/SE1994000594
申请日：1994-06-16
申请人： FERRING B.V. , NILSSON, Anders , OLSSON, Håkan , SÖDERBERG-AHLM, Christina , TROJNAR, Jerzy
发明人： FERRING B.V.
IPC分类号： C07K07/16
CPC分类号： C07K7/16 , A61K38/00 , Y10S514/807 , Y10S514/866 , Y10S930/15
摘要： Vasopressin analogues of formula (I) wherein X is (S)-2-amino-2-methyl-butanoic acid (C alpha MeAbu) or Valine (Val), Y is Thienylalanine (Thi) or Methionine (Met), Z is D-Phenylalanine (D-Phe) or D-Thienylalanine (Thi) or D-Tyrosine (D-Tyr), are disclosed. Pharmaceutical preparations comprising a vasopressin analogue of the invention as active ingredient are disclosed and exemplified by oral preparations, nasal preparations, and intravenous preparations. The vasopressin analogues of the invention are intended for use as a medicament, specially an antidiuretic agent. The antidiuretic agent is preferably used for the treatment of diabetes insipidus or enuresis.
摘要翻译：式（I）的加压素类似物，其中X是（S）-2-氨基-2-甲基 - 丁酸（CαMeAbu）或缬氨酸（Val），Y是噻吩丙氨酸（Thi）或甲硫氨酸（Met），Z是D 苯丙氨酸（D-Phe）或D-噻吩丙氨酸（Thi）或D-酪氨酸（D-Tyr）。包含本发明的加压素类似物作为活性成分的药物制剂通过口服制剂，鼻制剂和静脉内制剂来公开和举例。本发明的血管加压素类似物旨在用作药物，特别是抗利尿剂。抗利尿剂优选用于治疗尿崩症或遗尿症。

7. 发明申请

WO1992000996A1 DERIVATIVES OF PITUITARY POSTERIOR LOBE HORMONES 审中-公开
标题翻译：临床前列腺激素衍生物
公开(公告)号：WO1992000996A1
公开(公告)日：1992-01-23
申请号：PCT/SE1991000477
申请日：1991-07-04
申请人： FERRING AB , TROJNAR, Jerzy , LEBL, Michal , MELIN, Per
发明人： FERRING AB
IPC分类号： C07K07/16
CPC分类号： C07K7/16 , A61K38/00
摘要： Derivatives of pituitary posterior lobe hormones, more precisely new vasotocin derivatives, are disclosed. The new vasotocin derivatives are comprised by formula (I), wherein A = Mpa or Hmp, B = D-Tyr, D-Tyr(Et), D-Phe, D-Phe(p-Et) or D-Trp, C = Thr, Val or Hgn, D = Cys or alpha -Abu, E = Pro or a peptide bond, F = (a), wherein m = 0-6, n = 0-6, L = H, C00H, CO-NH2 or CH2-OH, K = H, (b) or a D- or L-amino acid residue with the proviso that L is not H when A is Mpa, C is Thr or Val and D is Cys. Further, pharmaceutical compositions including the new vasotocin derivatives and being preferably in a form suitable for intravenous, intranasal or intraintestinal administration, are described. The compositions are especially intended for use in the therapeutic treatment of excessive uterus muscle contractions.
摘要翻译：垂体后叶激素的衍生物，更准确地说是新的血管生成衍生物。新的血管生成衍生物由式（I）组成，其中A = Mpa或Hmp，B = D-Tyr，D-Tyr（Et），D-Phe，D-Phe（p-Et）或D-Trp，C = Thr，Val或Hgn，D = Cys或α-Abu，E = Pro或肽键，F =（a），其中m = 0-6，n = 0-6，L = H，C00H， NH 2或CH 2 -OH，K = H，（b）或D-或L-氨基酸残基，条件是当A为Mpa时L不为H，C为Thr或Val，D为Cys。此外，描述了包含新的血管舒芬素衍生物并且优选为适于静脉内，鼻内或肠内给药的形式的药物组合物。组合物特别用于治疗过度子宫肌肉收缩的治疗。

8. 发明申请

WO1990013567A1 NEW HUMAN PARVOVIRUS PEPTIDES WITH DISULFIDE BRIDGE FOR IMMUNIZATION OR DIAGNOSIS 审中-公开
标题翻译：用于免疫或诊断的新型人造血管病毒肽
公开(公告)号：WO1990013567A1
公开(公告)日：1990-11-15
申请号：PCT/SE1990000276
申请日：1990-04-25
申请人： FERRING DIAGNOSTICA AB , TROJNAR, Jerzy , WAHREN, Britta , FRIDELL, Eva
发明人： FERRING DIAGNOSTICA AB
IPC分类号： C07K07/10
CPC分类号： C07K14/005 , A61K39/00 , C12N2750/14222
摘要： An artificial peptide having an amino acid sequence which corresponds to a naturally occurring amino acid sequence of a human parvovirus comprising an epitope and which further has two cysteine residues located on each side of said epitope, and further having a sulphur bridge between said two cysteine residues, which has been formed by a chemical oxidation step, is described. Furthermore, an artificial antigen which reacts with antibodies induced by a human parvovirus is described. Said antigen mainly consists of an artificial peptide according to the invention. Additionally, a method of detecting antibodies induced by a human parvovirus in a sample of body fluid, wherein said sample is subjected to an immunoassay, especially ELISA, and wherein an artificial antigen according to the invention is used as a diagnostic antigen, is described. A diagnostic immunoassay kit for said method is also described. Finally, a vaccine composition comprising, as an immunizing component, at least one antigen according to the invention, is described.
摘要翻译：一种人造肽，其具有对应于包含表位的人细小病毒的天然存在的氨基酸序列的氨基酸序列，并且还具有位于所述表位的每一侧上的两个半胱氨酸残基，并且在所述两个半胱氨酸残基之间还具有硫桥，其通过化学氧化步骤形成。此外，描述了与人细小病毒诱导的抗体反应的人造抗原。所述抗原主要由根据本发明的人造肽组成。另外，本发明描述了检测体液样品中的人细小病毒诱导的抗体的方法，其中对所述样品进行免疫测定，特别是ELISA，其中使用本发明的人造抗原作为诊断抗原。还描述了用于所述方法的诊断免疫测定试剂盒。最后，描述了包含作为免疫组分的至少一种根据本发明的抗原的疫苗组合物。

9. 发明申请

WO1988010266A1 CYSTEINE PROTEINASE INHIBITOR 审中-公开
标题翻译： CYSTEINE蛋白酶抑制剂
公开(公告)号：WO1988010266A1
公开(公告)日：1988-12-29
申请号：PCT/SE1988000334
申请日：1988-06-17
申请人： GRUBB, Anders , ABRAHAMSON, Magnus , TROJNAR, Jerzy
IPC分类号： C07K05/04
CPC分类号： C07K5/0808 , Y02P20/55
摘要： New compounds which are cysteine proteinase inhibitors of the formula B - A - C wherein B = Pro-Arg-Leu-Val-Gly-, Arg-Leu-Val-Gly-, Leu-Val-Gly-, or Val-Gly-, or zero; the N-terminal amino acid optionally having a protective group, A = a reactive group capable of specifically reacting with free-SH groups, C = -Gly-Pro-Met-Asp-Ala; -Gly-Pro-Met-Asp; -Gly-Pro-Met; or -Gly-Pro, or zero; with the proviso that B and C are not both zero.
摘要翻译：作为式B-A-C的半胱氨酸蛋白酶抑制剂的新化合物，其中B = Pro-Arg-Leu-Val-Gly-，Arg-Leu-Val-Gly-，Leu-Val-Gly-或Val-Gly- ，或零; 任选具有保护基团的N-末端氨基酸，A =能够与游离SH基团特异性反应的反应性基团，C = -Gly-Pro-Met-Asp-Ala; -Gly-PRO-MET-天冬氨酸; -Gly-PRO-Met的; 或-Gly-Pro，或零; 条件是B和C都不为零。

10. 发明申请

WO2007139921A2 N-OXIDES OF KAPPA OPIOID RECEPTOR PEPTIDES 审中-公开
标题翻译： KAPPA阿片受体肽的N-氧化物
公开(公告)号：WO2007139921A2
公开(公告)日：2007-12-06
申请号：PCT/US2007/012463
申请日：2007-05-25
申请人： CARA THERAPEUTICS, INC. , JUNIEN, Jean-Louis , RIVIERE, Pierre, J., M. , SCHTEINGART, Claudio, D. , DIAZ, Javier, S. , TROJNAR, Jerzy, A. , VANDERAH, Todd, W. , LEWIS, Michael, E.
发明人： JUNIEN, Jean-Louis , RIVIERE, Pierre, J., M. , SCHTEINGART, Claudio, D. , DIAZ, Javier, S. , TROJNAR, Jerzy, A. , VANDERAH, Todd, W. , LEWIS, Michael, E.
IPC分类号： C07K5/10 , C07K5/107 , C07K5/117 , A61K38/07 , A61P29/00 , A61P13/10 , A61P1/00 , A61P17/04 , A61P37/00
CPC分类号： C07K5/1016 , A61K38/00
摘要： Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4- picolyl-N-oxide. A preferred compound, which has an affinity for the KOR at least 1,000 times its affinity for the mu opioid receptor and an IC50 for CYP3 A4 of greater than about 10 micromolar, is H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide
摘要翻译：对于κ阿片样物质受体（KOR）与μ-阿片样物质受体显示出高选择性的某些肽，并且很少或没有CYP3A4抑制活性，包括具有C-末端的四个D-异构体氨基酸残基的四肽，其是N-氧化物取代的酰胺如HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基-N-氧化物。 HD-Phe-D-Phe-D-Nle-D-D对于KOR具有对μ-阿片样物质受体的亲和力至少1000倍的亲和力以及大于约10微摩尔的CYP3A4的IC 50的优选化合物，精氨酸-NH-4-吡啶甲基-N-氧化物

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