RU93004994A - Продукты, применение и способ получения антагонистов гормона, стимулирующего выделение лютеинизирующего гормона - Google Patents
Продукты, применение и способ получения антагонистов гормона, стимулирующего выделение лютеинизирующего гормонаInfo
- Publication number
- RU93004994A RU93004994A RU93004994/04A RU93004994A RU93004994A RU 93004994 A RU93004994 A RU 93004994A RU 93004994/04 A RU93004994/04 A RU 93004994/04A RU 93004994 A RU93004994 A RU 93004994A RU 93004994 A RU93004994 A RU 93004994A
- Authority
- RU
- Russia
- Prior art keywords
- stimulating
- release
- hormone
- products
- application
- Prior art date
Links
- 230000004936 stimulating Effects 0.000 title claims 2
- 229940040129 Luteinizing Hormone Drugs 0.000 title 1
- 102000009151 Luteinizing Hormone Human genes 0.000 title 1
- 108010073521 Luteinizing Hormone Proteins 0.000 title 1
- 239000003667 hormone antagonist Substances 0.000 title 1
- 125000000030 D-alanine group Chemical group [H]N([H])[C@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 2
- 210000001009 Nucleus accumbens Anatomy 0.000 claims 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims 2
- 125000000052 D-arginine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C([H])([H])C([H])([H])N([H])C(N([H])[H])=N[H] 0.000 claims 1
- 102100000899 GNRH1 Human genes 0.000 claims 1
- 108010084340 Gonadotropin-Releasing Hormone Proteins 0.000 claims 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
- XLXSAKCOAKORKW-KPKRHBJMSA-N N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl] Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-KPKRHBJMSA-N 0.000 claims 1
- 230000003042 antagnostic Effects 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000002513 anti-ovulatory Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229960001340 histamine Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000004048 modification Effects 0.000 claims 1
- 238000006011 modification reaction Methods 0.000 claims 1
- 239000007858 starting material Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Claims (1)
- Это изобретение включает два аспекта: способ получения антагонистов LHRH и продукты, полученные с использованием вышеназванного способа. Используя (NAc -D2Nal1, DpClPhe2, D3Pal3, Ser4, Tyr5, DArg6, Leu7, Arg8, Pro9, DAla1 0)NH в качестве исходного соединения, получены серии новых аналогов, выражаемых (NAc - D2Nal1, AA2, AA3, Ser4, AA5, AA6, Leu7, AA8, Pro9, DAla1 0)NH2 с помощью тонких модификаций как липофильного участка, так и щелочного участка молекулы исходного соединения. Таким образом, высокая антиовуляторная активность исходного вещества может быть сохранена и активность по стимуляции выделения гистамина может быть снижена до такого уровня, чтобы удовлетворять клиническим требованиям.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN90108955.9 | 1990-11-10 | ||
| CN90108955A CN1036343C (zh) | 1990-11-10 | 1990-11-10 | 新促黄体生成素释放激素拮抗类似物的制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU93004994A true RU93004994A (ru) | 1996-03-10 |
| RU2123499C1 RU2123499C1 (ru) | 1998-12-20 |
Family
ID=4881223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU93004994A RU2123499C1 (ru) | 1990-11-10 | 1991-11-08 | Аналоги антагонистов lhrh и способы их получения |
Country Status (29)
| Country | Link |
|---|---|
| EP (1) | EP0564466B1 (ru) |
| KR (1) | KR100244624B1 (ru) |
| CN (1) | CN1036343C (ru) |
| AT (1) | ATE149520T1 (ru) |
| AU (1) | AU662496B2 (ru) |
| CA (1) | CA2095932C (ru) |
| CZ (1) | CZ284168B6 (ru) |
| DE (1) | DE69125024T2 (ru) |
| DK (1) | DK0564466T3 (ru) |
| EE (1) | EE03141B1 (ru) |
| ES (1) | ES2100965T3 (ru) |
| FI (1) | FI933156A (ru) |
| GR (1) | GR3023389T3 (ru) |
| HR (1) | HRP920585B1 (ru) |
| IE (1) | IE913915A1 (ru) |
| LT (1) | LT3971B (ru) |
| LV (1) | LV10106B (ru) |
| NO (1) | NO931697L (ru) |
| NZ (1) | NZ240505A (ru) |
| PH (1) | PH31178A (ru) |
| PL (1) | PL170564B1 (ru) |
| PT (1) | PT99458B (ru) |
| RU (1) | RU2123499C1 (ru) |
| SI (1) | SI9111779B (ru) |
| SK (1) | SK281319B6 (ru) |
| UA (1) | UA41300C2 (ru) |
| WO (1) | WO1992008733A1 (ru) |
| YU (1) | YU48831B (ru) |
| ZA (1) | ZA918847B (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3568952B2 (ja) * | 1992-12-18 | 2004-09-22 | アボット・ラボラトリーズ | ５位及び６位に修飾アミノアシル残基を有するｌｈｒｈ拮抗薬 |
| DE4305225A1 (de) * | 1993-02-19 | 1994-08-25 | Asta Medica Ag | Neues Herstellverfahren für Cetrorelix Lyophilisat |
| US6828415B2 (en) | 1993-02-19 | 2004-12-07 | Zentaris Gmbh | Oligopeptide lyophilisate, their preparation and use |
| DE4338015A1 (de) * | 1993-11-08 | 1995-05-11 | Asta Medica Ag | Verwendung von D-glucopyranuronsäuren und deren Derivaten zum Einbau in pharmakologisch wirksame Peptide und deren Salze |
| US5843901A (en) * | 1995-06-07 | 1998-12-01 | Advanced Research & Technology Institute | LHRH antagonist peptides |
| US5968547A (en) | 1997-02-24 | 1999-10-19 | Euro-Celtique, S.A. | Method of providing sustained analgesia with buprenorphine |
| CN101037472B (zh) * | 2006-03-14 | 2013-03-27 | 中国人民解放军军事医学科学院毒物药物研究所 | 具有低组胺释放作用的促黄体生成素释放激素拮抗剂 |
| CN102675418B (zh) * | 2011-03-15 | 2016-04-20 | 中国人民解放军军事医学科学院毒物药物研究所 | Lhrh拮抗剂衍生物、其制备方法及用途 |
| CN103524599B (zh) * | 2012-07-05 | 2016-04-20 | 中国人民解放军军事医学科学院毒物药物研究所 | 环肽lhrh拮抗剂衍生物及其药物用途 |
| CN104418936B (zh) * | 2013-08-20 | 2018-06-05 | 中国人民解放军军事医学科学院毒物药物研究所 | Lhrh拮抗剂衍生物及其药物用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4801577A (en) * | 1987-02-05 | 1989-01-31 | Syntex (U.S.A.) Inc. | Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists |
| US4851385A (en) * | 1987-07-15 | 1989-07-25 | Indiana University Foundation | LHRH antagonist analogs having low histamine-release activity |
-
1990
- 1990-11-10 CN CN90108955A patent/CN1036343C/zh not_active Expired - Lifetime
-
1991
- 1991-11-07 NZ NZ240505A patent/NZ240505A/xx not_active IP Right Cessation
- 1991-11-07 ZA ZA918847A patent/ZA918847B/xx unknown
- 1991-11-08 AU AU88612/91A patent/AU662496B2/en not_active Ceased
- 1991-11-08 IE IE391591A patent/IE913915A1/en not_active Application Discontinuation
- 1991-11-08 CZ CZ93848A patent/CZ284168B6/cs not_active IP Right Cessation
- 1991-11-08 DK DK91919435.7T patent/DK0564466T3/da active
- 1991-11-08 PT PT99458A patent/PT99458B/pt not_active IP Right Cessation
- 1991-11-08 DE DE69125024T patent/DE69125024T2/de not_active Expired - Lifetime
- 1991-11-08 WO PCT/EP1991/002110 patent/WO1992008733A1/en active IP Right Grant
- 1991-11-08 ES ES91919435T patent/ES2100965T3/es not_active Expired - Lifetime
- 1991-11-08 KR KR1019930701418A patent/KR100244624B1/ko not_active IP Right Cessation
- 1991-11-08 PH PH43428A patent/PH31178A/en unknown
- 1991-11-08 RU RU93004994A patent/RU2123499C1/ru not_active IP Right Cessation
- 1991-11-08 SK SK453-93A patent/SK281319B6/sk unknown
- 1991-11-08 SI SI9111779A patent/SI9111779B/sl not_active IP Right Cessation
- 1991-11-08 UA UA94030668A patent/UA41300C2/ru unknown
- 1991-11-08 AT AT91919435T patent/ATE149520T1/de not_active IP Right Cessation
- 1991-11-08 EP EP91919435A patent/EP0564466B1/en not_active Expired - Lifetime
- 1991-11-08 YU YU177991A patent/YU48831B/sh unknown
- 1991-11-08 CA CA002095932A patent/CA2095932C/en not_active Expired - Lifetime
-
1992
- 1992-09-29 HR HR920585A patent/HRP920585B1/xx not_active IP Right Cessation
- 1992-10-27 LV LVP-92-175A patent/LV10106B/en unknown
-
1993
- 1993-05-10 NO NO93931697A patent/NO931697L/no not_active Application Discontinuation
- 1993-05-10 PL PL91295427A patent/PL170564B1/pl unknown
- 1993-07-09 FI FI933156A patent/FI933156A/fi not_active Application Discontinuation
- 1993-12-03 LT LTIP1513A patent/LT3971B/lt not_active IP Right Cessation
-
1994
- 1994-10-25 EE EE9400178A patent/EE03141B1/xx not_active IP Right Cessation
-
1997
- 1997-05-09 GR GR970401042T patent/GR3023389T3/el unknown
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