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1. 发明授权

US6051555A Stimulating sexual response in females 有权
标题翻译：刺激女性的性反应
公开(公告)号：US6051555A
公开(公告)日：2000-04-18
申请号：US179225
申请日：1998-10-27
申请人： Mac E. Hadley
发明人： Mac E. Hadley
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61K49/00 , A61P13/02 , A61P15/00 , A61P15/10 , C07K7/06 , C07K14/68 , C07K14/695
CPC分类号： C07K14/68 , C07K14/6955 , A61K38/00 , Y10S436/811
摘要： The present invention is directed to a series of peptides which may be used for stimulating sexual response in females.
摘要翻译：本发明涉及可用于刺激女性性反应的一系列肽。

2. 发明公开

EP0461696A1 Crystalline polypeptides with corticotropic activity 失效
标题翻译： Kristallinische Polypeptide mit corticotroperAktivität。
公开(公告)号：EP0461696A1
公开(公告)日：1991-12-18
申请号：EP91201319.0
申请日：1991-05-31
申请人： Akzo Nobel N.V.
发明人： van Nispen, Johannes Wilhelmus Franciscus Maria , van de Oetelaar, Petrus Johannes Maria , Janssen, Wilhelmus Petrus Andreas
IPC分类号： C07K7/38 , A61K37/40
CPC分类号： C07K14/6955 , A61K38/00
摘要： Disclosed is a method of obtaining an acid addition salt, crystalline compound of the formula:

H-MetO₂-Glu-His-Phe-D-Lys-Phe-OH.

The resulting crystalline hexapeptide salt has better intranasal absorption characteristics in comparison to amorphous hexapeptide. The method includes: a) dissolving relatively pure hexapeptide into an aqueous acidic solvent; b) concentrating the resulting solution under reduced pressure at an elevated temperature; c) measuring the pH of the concentrated solution, and if the pH is between 4.5 and 4.8, then d) maintaining the temperature of the concentrated solution between 6 and 20 o C, if the measured pH of the concentrated solution is lower than 4.5, then adding water to the solution and repeating step b) until a pH of 4.5 to 4.8 is attained; and then e) removing the crystals from the concentrated solution by filtration at lower temperatures. Previously obtained "seed" crystals comprising the acid addition salt of the hexapeptide may be used to hasten the process. Once obtained, the crystalline compound may be used in the treatment or prevention of neuropathies or dementia.
摘要翻译：公开了获得酸加成盐的方法，即下式的结晶化合物：H-MetO 2 -Glu-His-Phe-D-Lys-Phe-OH。与无定形六肽相比，所得结晶六肽盐具有更好的鼻内吸收特征。该方法包括：a）将相对纯的六肽溶于含水的酸性溶剂中; b）在升高的温度下将所得溶液在减压下浓缩; c）测量浓缩溶液的pH，如果pH在4.5至4.8之间，则d）将浓缩溶液的温度保持在6至20℃之间，如果浓缩溶液的测量pH低于 4.5，然后向溶液中加水并重复步骤b），直至达到4.5至4.8的pH; 然后e）在较低温度下过滤从浓缩溶液中除去晶体。先前获得的包含六肽的酸加成盐的“晶种”晶体可用于加速该方法。一旦获得，结晶化合物可用于治疗或预防神经病或痴呆症。

3. 发明公开

EP0381070A1 Synthetic amphiphilic glycoconjugates for neurological use 失效
标题翻译： Synthetische amphiphilische Glykoconjugatefürneurologische Verwendung。
公开(公告)号：EP0381070A1
公开(公告)日：1990-08-08
申请号：EP90101569.3
申请日：1990-01-26
申请人： FARMHISPANIA S.A.
发明人： Butelman, Edoardo , Sirtori, Cesare
IPC分类号： C07H15/04 , A61K31/70 , C07K9/00 , A61K37/02 , C07H15/06 , C07H15/26 , C07H19/16
CPC分类号： C07H15/04 , C07H7/033 , C07H15/06 , C07H15/26 , C07H19/16 , C07K14/685 , C07K14/69 , C07K14/6955
摘要： Chemically and sterically pure synthetic amphiphilic glycoconjugates for neurological use of general formula (I):
in which:
the saccharide ring represents a monosaccharide such as glucose, galactose or mannose;
X represents O or NH and, when X represents O, R is a group derived from choline whereas, when X represents NH, R is a group derived from an amino acid or peptide; R′ represents a saturated or unsaturated linear or branched C₈-C₁₈ aliphatic chain, or a
group or a
group where m is between 7 and 17;
n is a whole number from 1 to 5.
摘要翻译：化学和空间纯的用于神经学用途的通式（I）的合成两亲糖缀合物：其中：糖环表示单糖如葡萄糖，半乳糖或甘露糖; X表示O或NH，当X表示O时，R是来自胆碱的基团，而当X表示NH时，R是衍生自氨基酸或肽的基团; R min表示饱和或不饱和的直链或支链C 8 -C 18脂族链，或其中m为7至17的基团或基团; n是从1到5的整数

4. 发明申请

WO1994022460A1 DIAGNOSIS AND TREATMENT OF ERECTILE DYSFUNCTION 审中-公开
标题翻译：诊断和治疗溃疡性功能障碍
公开(公告)号：WO1994022460A1
公开(公告)日：1994-10-13
申请号：PCT/US1994003677
申请日：1994-04-04
申请人： UNIVERSITY PATENTS, INC.
发明人： UNIVERSITY PATENTS, INC. , HADLEY, Mac, E.
IPC分类号： A61K37/00
CPC分类号： C07K14/68 , A61K38/00 , C07K14/6955 , Y10S436/811
摘要： The present invention is directed to a series of peptides which may be used for the diagnosis and treatment of psychogenic sexual dysfunction in the male.
摘要翻译：本发明涉及可用于诊断和治疗男性心理性功能障碍的一系列肽。

5. 发明申请

WO1982003388A1 PEPTIDES WITH NERVE-REGENERATING PROPERTIES 审中-公开
标题翻译：具有神经再生特性的肽
公开(公告)号：WO1982003388A1
公开(公告)日：1982-10-14
申请号：PCT/EP1982000079
申请日：1982-04-05
申请人： AKZO NV , GISPEN WILLEM HENDRIK
发明人： AKZO NV
IPC分类号： C07C103/52
CPC分类号： C07K14/6955 , A61K38/00 , C07K14/695
摘要： Use of the peptides of the general formula: A-B-L-Phe (or L-Ala)-D-Lys-L-Phe-Z-OH, where A represents one of the following groups: H-L-Met, H-L-Met(O), H-L-Met(O2), desamino-Met, desamino-Met(O) or desamino-Met(O2), B represents one of the following di-peptide fragments: Glu-His or Ala-Ala, where one amino acid residue of this di-peptide fragment can occur in the D form, and Z is either absent, or represents the amino acid residue Gly, or is the peptide fragment (10-16)-ACTH, where the amino acid L-Lys may be replaced, if desired, by D-Lys at position 11 of the (10-16)-ACTH fragment, and the functional derivatives thereof in promoting axonal regeneration.
摘要翻译：使用以下通式的肽：ABL-Phe（或L-Ala）-D-Lys-L-Phe-Z-OH，其中A代表下列基团之一：HL-Met，HL-Met（O），HL-Met（O2），desamino-Met，desamino-Met（O）或desamino-Met（O2），B代表以下二肽片段之一：Glu-His或Ala-Ala，其中一个氨基酸残基该二肽片段可以以D形式出现，Z不存在，或表示氨基酸残基Gly，或是肽片段（10-16）-ACTH，其中可以替换氨基酸L-Lys 如果需要，由（10-16）-ACTH片段的第11位的D-Lys及其功能衍生物促进轴突再生。

6. 发明授权

US4550099A Peptides with nerve-regenerating properties 失效
标题翻译：具有神经再生特性的肽
公开(公告)号：US4550099A
公开(公告)日：1985-10-29
申请号：US658544
申请日：1984-10-09
申请人： Willem H. Gispen
发明人： Willem H. Gispen
IPC分类号： A61K38/00 , A61P25/00 , A61P25/28 , A61P25/30 , C07K14/00 , C07K14/695 , A61K37/00
CPC分类号： C07K14/6955 , C07K14/695 , A61K38/00
摘要： The present invention relates to the use of the peptides of the general formula:A--B--L--Phe (or L--Ala)--D--Lys--L--Phe--Z--OH, IwhereA represents one of the following groups: H--L--Met, H--L--Met(O), H--L--Met(O.sub.2), desamino-Met, desamino-Met(O) or desamino-Met(O.sub.2),B represents one of the following di-peptide fragments: Glu--His or Ala--Ala, where one amino acid residue of this di-peptide fragment can occur in the D form, andZ is either absent, or represents the amino acid residue Gly, or is the peptide fragment (10-16)--ACTH, where the amino acid L--Lys may be replaced, if desired, by D--Lys at position 11 of the (10-16)--ACTH fragment,and the functional derivatives thereof in promoting axonal regeneration.
摘要翻译：本发明涉及以下通式的肽：ABL-Phe（或L-Ala）-D-Lys-L-Phe-Z-OH，I的用途，其中A代表以下基团之一：HL-Met ，HL-Met（O），HL-Met（O2），desamino-Met，desamino-Met（O）或desamino-Met（O 2），B代表以下二肽片段之一：Glu-His或Ala- Ala，其中该二肽片段的一个氨基酸残基可以以D形式出现，Z不存在，或表示氨基酸残基Gly，或是肽片段（10-16）-ACTH，其中氨基如果需要，酸性L-Lys可以被（10-16）-ACTH片段的第11位的D-Lys和其功能衍生物替代，以促进轴突再生。

7. 发明授权

US4457864A Synthetic analogues of .alpha.-melanotropin 失效
标题翻译： α-促黄体素的合成类似物
公开(公告)号：US4457864A
公开(公告)日：1984-07-03
申请号：US314387
申请日：1981-10-23
申请人： Victor J. Hruby , Mac E. Hadley , Christopher B. Heward , Tomi K. Sawyer
发明人： Victor J. Hruby , Mac E. Hadley , Christopher B. Heward , Tomi K. Sawyer
IPC分类号： A61K38/00 , C07K14/695 , C07C103/52
CPC分类号： C07K14/6955 , A61K38/00
摘要： Analogues of the tridecapeptide hormone, .alpha.-melanotropin (a-melanocyte stimulating hormone, .alpha.-MSH) of the formula:Ac-Ser.sup.1 -Tyr.sup.2 -Ser.sup.3 -Y.sup.4 -Glu.sup.5 -His.sup.6 -X.sup.7 -Arg.sup.8 -Trp.sup.9 -Gly.sup.10 -Lys.sup.11 -Pro.sup.12 -Val.sup.13 -NH.sub.2wherein X and Y are amino acid residues and X is in a D-isomeric configuration. Preferred analogues, e.g. [Nle.sup.4, D-Phe.sup.7 ]-.alpha.-MSH, display increased in vitro and in vivo potency, prolongation and serum stability characteristics and may be covalently bonded to other elements or compounds (e.g., radioisotopes of iodine) without significant loss of biological activity.
摘要翻译：类似物：Ac-Ser1-Tyr2-Ser3-Y4-Glu5-His6-X7-Arg8-Trp9-Gly10-Lys11-Pro12-的三十肽肽激素，α-促黄体激素（a-黑素细胞刺激激素，α-MSH） Val13-NH2，其中X和Y是氨基酸残基，X是D-异构构型。优选的类似物，例如 [Nle4，D-Phe7]-α-MSH显示增加的体外和体内效力，延长和血清稳定性特征，并且可以共价键合到其他元素或化合物（例如碘的放射性同位素），而不会显着丧失生物活性。

8. 发明授权

US4193915A Contraceptive, antibody generating, polypeptides 失效
标题翻译：避孕药，产生抗体，多肽
公开(公告)号：US4193915A
公开(公告)日：1980-03-18
申请号：US896225
申请日：1978-04-13
申请人： Kenneth W. McKerns
发明人： Kenneth W. McKerns
IPC分类号： A61K38/00 , C07K14/59 , C07K14/695 , C07C103/52 , A61K37/00
CPC分类号： C07K14/59 , C07K14/6955 , A61K38/00 , Y10S514/80 , Y10S930/11 , Y10S930/13
摘要： Polypeptides D-Ser-Arg-Tyr-Gly-Pro-Val-Gly-Val-NH.sub.2, D-Ser-Arg-Ala-Tyr-Pro-Thr-Pro-Ala-Arg-Ser-Lys-Lys-NH.sub.2, D-Ser-Arg-Tyr-Gly-Lys-Pro-Val-Gly-Lys-Lys-Lys-Lys-NH.sub.2, D-Ser-Arg-Tyr-Gly-Lys-Pro-Val-Arg-Ser-Lys-Lys-NH.sub.2, D-Ser-Arg-Tyr-Gly-Pro-Val-NH.sub.2, D-Ser-Arg-Tyr-Gly-Lys-Pro-Val-Gly-Lys-Lys-Val-NH.sub.2, D-Ser-Arg-Leu-Pro-Gly-Pro-Ser-NH.sub.2, D-Ser-Arg-Val-Leu-Val-Gly-Val-NH.sub.2, D-Ser-Arg-Val-Leu-Pro-Val-NH.sub.2, D-Ser-Arg-Ala-Tyr-Pro-Thr, D-Ser-Arg-Val-Leu-Gln-Gly-Val-NH.sub.2, D-Ser-Arg-Ala-Tyr-Pro-Arg-Leu-Pro-Gly-Pro-NH.sub.2, D-Ser-Arg-Ala-Tyr-Pro-Arg-Val-Leu-Gln-Gly-Val-NH.sub.2, D-Ser-Arg-Ala-Tyr-Pro-Arg-Val-Leu-Pro-Val-NH.sub.2, are useful as contraceptives.
摘要翻译：多肽D-Ser-Arg-Tyr-Gly-Pro-Val-Gly-Val-NH2，D-Ser-Arg-Ala-Tyr-Pro-Thr-Pro-Ala-Arg-Ser-Lys-Lys-NH2 -Ser-Arg-Tyr-Gly-Lys-Pro-Val-Gly-Lys-Lys-Lys-Lys-NH2，D-Ser-Arg-Tyr-Gly-Lys-Pro-Val-Arg-Ser-Lys-Lys -NH2，D-Ser-Arg-Tyr-Gly-Pro-Val-NH2，D-Ser-Arg-Tyr-Gly-Lys-Pro-Val-Gly-Lys-Lys-Val-NH2， -Leu-Pro-Gly-Pro-Ser-NH2，D-Ser-Arg-Val-Leu-Val-Gly-Val-NH2，D-Ser-Arg-Val-Leu-Pro-Val-NH2，D-Ser -Arg-Ala-Tyr-Pro-Thr，D-Ser-Arg-Val-Leu-Gln-Gly-Val-NH2，D-Ser-Arg-Ala-Tyr-Pro-Arg-Leu-Pro-Gly-Pro -NH2，D-Ser-Arg-Ala-Tyr-Pro-Arg-Val-Leu-Gln-Gly-Val-NH2，D-Ser-Arg-Ala-Tyr-Pro-Arg-Val-Leu-Pro-Val -NH2可用作避孕药具。

9. 发明授权

US3873510A Peptides of ACTH activity containing {60 -aminooxy carboxylic acid on the N-terminal moiety, and a process for the preparation thereof 失效
标题翻译：在N-末端部分含有{60-氨基氧基羧酸的ACTH活性肽及其制备方法
公开(公告)号：US3873510A
公开(公告)日：1975-03-25
申请号：US38854673
申请日：1973-08-15
申请人： RICHTER GEDEON VEGYESZET
发明人： KISFALUDY LAJOS , LOW MIKLOS , DANCSI LAJOS , SCHON ISTVAN , SZIRTES TAMAS , NYEKI OLGA , SZIRMAI MARIA , SZPORNY LASZLO , HAJOS GYORGY
IPC分类号： C07K14/575 , A61K38/00 , A61K38/22 , C07K1/06 , C07K14/695 , C07C103/52 , A61K17/06
CPC分类号： C07K14/6955 , A61K38/00 , C07K14/695 , Y10S514/805
摘要： Novel peptides of ACTH activity, having a complete ACTH sequence from the N-terminal amino acid at least to the sixteenth amino acid, but containing optionally other amino acids in the place of the individual amino acids of the ACTH sequence, and always containing an Alpha -aminooxy acid in the place of the first amino acid have been prepared by deblocking the appropriate protected peptide derivatives. The new compounds, as well as their acid addition salts, derivatives or complexes possess potent ACTH activities and are resistant to enzymatic decomposition. They can be used in therapy with great advantages.
摘要翻译：具有ACTH活性的新肽，具有至少至第十六氨基酸的N-末端氨基酸的完整ACTH序列，但含有任选的其它氨基酸代替ACTH序列的各个氨基酸，并且总是含有α - 氨基氧酸代替第一个氨基酸已经通过解封合适当的保护肽衍生物来制备。

10. 发明公开

EP0696919A4 DIAGNOSIS AND TREATMENT OF ERECTILE DYSFUNCTION 失效
标题翻译： DIAGNOSE UND BEHANDLUNG VON EREKTILENFUNKTIONSSTÖRUNGEN
公开(公告)号：EP0696919A4
公开(公告)日：1998-03-11
申请号：EP94912948
申请日：1994-04-04
申请人： COMPETITIVE TECH INC
发明人： HADLEY MAC E
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61K49/00 , A61P13/02 , A61P15/00 , A61P15/10 , C07K7/06 , C07K14/68 , C07K14/695 , C07K7/00
CPC分类号： C07K14/68 , A61K38/00 , C07K14/6955 , Y10S436/811
摘要： The present invention is directed to a series of peptides which may be used for the diagnosis and treatment of psychogenic sexual dysfunction in the male.
摘要翻译：本发明涉及可用于刺激女性性反应的一系列肽。

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