RU98104253A - Новые опиоидные пептиды - Google Patents
Новые опиоидные пептидыInfo
- Publication number
- RU98104253A RU98104253A RU98104253/04A RU98104253A RU98104253A RU 98104253 A RU98104253 A RU 98104253A RU 98104253/04 A RU98104253/04 A RU 98104253/04A RU 98104253 A RU98104253 A RU 98104253A RU 98104253 A RU98104253 A RU 98104253A
- Authority
- RU
- Russia
- Prior art keywords
- phe
- compound according
- tyr
- arg
- ala
- Prior art date
Links
- 102000001490 Opioid Peptides Human genes 0.000 title 1
- 108010093625 Opioid Peptides Proteins 0.000 title 1
- 239000003399 opiate peptide Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 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 3
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 3
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 238000003379 elimination reaction Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 238000010532 solid phase synthesis reaction Methods 0.000 claims 1
Claims (16)
1. Соединение формулы (1):
a также его соли, производные и аналоги,
где R1 - Туr или 2'6'-диметилтирозин, или его производное или аналог;
R2 - D-Ala или D-Arg;
R3 - Phe(p-F);
R4 - Phe или Phe(p-F);
X - H или C1-6алкил;
Y и Z - независимо представляют H, аралкил или C1-6алкил.
a также его соли, производные и аналоги,
где R1 - Туr или 2'6'-диметилтирозин, или его производное или аналог;
R2 - D-Ala или D-Arg;
R3 - Phe(p-F);
R4 - Phe или Phe(p-F);
X - H или C1-6алкил;
Y и Z - независимо представляют H, аралкил или C1-6алкил.
2. Соединение по п. 1, где R2 представлен D-Ala.
3. Соединение по п. 1, где R2 представлен D-Arg.
4. Соединение по п. 1, где R4 представлен Phe.
5. Соединение по п. 4, где R2 представлен D-Ala.
6. Соединение по п. 4, где R2 представлен D-Arg.
7. Соединение по любому из пп. 1-6, где Х представляет Н, a Y и Z оба представляют Н.
8. Соединение по п. 1, выбранное из:
H-Tyr-D-Ala-Phe(p-F)-Phe(p-F)-NH2;
H-Tyr-D-Ala-Phe(p-F)-Phe-NH2.
H-Tyr-D-Ala-Phe(p-F)-Phe(p-F)-NH2;
H-Tyr-D-Ala-Phe(p-F)-Phe-NH2.
9. Соединение H-Tyr-D-Ala-Phe(p-F)-Phe-NH2.
10. Соединение по п. 1, выбранное из:
H-Tyr-D-Arg-Phe(p-F)-Phe(p-F)-NH2;
H-Tyr-D-Arg-Phe(p-F)-Phe-NH2.
H-Tyr-D-Arg-Phe(p-F)-Phe(p-F)-NH2;
H-Tyr-D-Arg-Phe(p-F)-Phe-NH2.
11. Соединение H-Tyr-D-Arg-Phe(p-F)-Phe-NH2.
12. Фармацевтическая композиция, включающая соединение по любому из пп. 1-11 в смеси с фармацевтически приемлемым носителем.
13. Фармацевтическая композиция, включающая соединение по п. 7, в смеси с фармацевтически приемлемым носителем.
14. Соединения по любому из пп. 1-6 и 8-11 полезные для изготовления препарата, эффективного для устранения боли.
15. Соединения по п. 7 полезные для изготовления препарата, эффективного для устранения боли.
16. Способ получения соединения по п. 1 путем твердофазного синтеза.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE9502877A SE9502877D0 (sv) | 1995-08-18 | 1995-08-18 | Novel opioid peptides |
| SE9502877-5 | 1995-08-18 | ||
| SE9503924-4 | 1995-11-07 | ||
| SE9503924A SE9503924D0 (sv) | 1995-08-18 | 1995-11-07 | Novel opioid peptides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU98104253A true RU98104253A (ru) | 1999-12-20 |
| RU2165432C2 RU2165432C2 (ru) | 2001-04-20 |
Family
ID=26662362
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU98104253/04A RU2165432C2 (ru) | 1995-08-18 | 1996-08-14 | Новые опиоидоподобные пептиды, способ их получения, фармацевтическая композиция |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US6337319B1 (ru) |
| EP (1) | EP0845003B1 (ru) |
| JP (1) | JPH11512086A (ru) |
| KR (1) | KR19990037677A (ru) |
| CN (1) | CN1200127A (ru) |
| AR (1) | AR003475A1 (ru) |
| AT (1) | ATE210148T1 (ru) |
| AU (1) | AU711862B2 (ru) |
| BR (1) | BR9610248A (ru) |
| CA (1) | CA2229797A1 (ru) |
| CZ (1) | CZ287299B6 (ru) |
| DE (1) | DE69617699T2 (ru) |
| DK (1) | DK0845003T3 (ru) |
| EE (1) | EE9800048A (ru) |
| ES (1) | ES2171224T3 (ru) |
| HU (1) | HUP9901209A3 (ru) |
| IL (1) | IL123258A (ru) |
| IS (1) | IS4664A (ru) |
| NO (1) | NO980592D0 (ru) |
| NZ (1) | NZ315809A (ru) |
| PL (1) | PL325113A1 (ru) |
| RU (1) | RU2165432C2 (ru) |
| SE (1) | SE9503924D0 (ru) |
| SK (1) | SK282469B6 (ru) |
| TR (1) | TR199800258T1 (ru) |
| TW (1) | TW424095B (ru) |
| WO (1) | WO1997007130A1 (ru) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030032774A1 (en) * | 1994-02-21 | 2003-02-13 | Astrazeneca Ab | Novel opioid peptides for the treatment of pain |
| US5885958A (en) * | 1997-03-25 | 1999-03-23 | Administrators Of The Tulane Educational Fund | Mu-opiate receptor peptides |
| SE9701718D0 (sv) * | 1997-05-07 | 1997-05-07 | Astra Ab | Analgesic peptidomimetic compounds |
| SE9800865D0 (sv) * | 1998-03-16 | 1998-03-16 | Astra Ab | New Process |
| WO2001013938A1 (fr) * | 1999-08-25 | 2001-03-01 | Daiichi Fine Chemical Co., Ltd. | Composition therapeutique pouvant etre administree par voie percutanee ou par les muqueuses |
| WO2001036006A1 (en) | 1999-11-19 | 2001-05-25 | Palatin Technologies, Inc. | Opioid metallopeptide compositions and methods |
| US7498297B2 (en) | 2000-07-18 | 2009-03-03 | Cornell Research Foundation | Medicinal uses of mu-opioid receptor agonists |
| JP2002069059A (ja) * | 2000-08-28 | 2002-03-08 | Teikoku Seiyaku Co Ltd | ピラジノン環を含む新規なオピオイドペプチド誘導体 |
| US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE10361596A1 (de) * | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| US20070048228A1 (en) | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
| DE102004032049A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Gegen Missbrauch gesicherte, orale Darreichungsform |
| AU2005286733B2 (en) * | 2004-09-23 | 2009-11-05 | Alexander Michalow | Methods for regulating neurotransmitter systems by inducing counteradaptations |
| US20080045610A1 (en) * | 2004-09-23 | 2008-02-21 | Alexander Michalow | Methods for regulating neurotransmitter systems by inducing counteradaptations |
| DE102005005449A1 (de) * | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| WO2006132925A2 (en) * | 2005-06-01 | 2006-12-14 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Method of amidated peptide biosynthesis and delivery in vivo: endomorphin-2 for pain therapy |
| EP1782819A1 (en) | 2005-11-03 | 2007-05-09 | Cognis IP Management GmbH | Oligopeptides and their use |
| NZ577107A (en) | 2006-11-10 | 2012-01-12 | Cara Therapeutics Inc | Synthetic peptide amide ligands of the kappa opiod receptor |
| US8236766B2 (en) | 2006-11-10 | 2012-08-07 | Cara Therapeutics, Inc. | Uses of synthetic peptide amides |
| US8906859B2 (en) | 2006-11-10 | 2014-12-09 | Cera Therapeutics, Inc. | Uses of kappa opioid synthetic peptide amides |
| US7842662B2 (en) | 2006-11-10 | 2010-11-30 | Cara Therapeutics, Inc. | Synthetic peptide amide dimers |
| US7713937B2 (en) | 2006-11-10 | 2010-05-11 | Cara Therapeutics, Inc. | Synthetic peptide amides and dimeric forms thereof |
| WO2009092601A1 (en) | 2008-01-25 | 2009-07-30 | Grünenthal GmbH | Pharmaceutical dosage form |
| MX2010012039A (es) * | 2008-05-09 | 2010-11-30 | Gruenenthal Gmbh | Proceso para la preparacion de una formulacion de polvo intermedia y una forma de dosificacion solida final bajo el uso de un paso de congelacion por rocio. |
| BR112012001547A2 (pt) | 2009-07-22 | 2016-03-08 | Gruenenthal Gmbh | forma de dosagem farmacêutica extrusada por fusão a quente |
| RU2567723C2 (ru) | 2009-07-22 | 2015-11-10 | Грюненталь Гмбх | Стабильная при окислении, прочная на излом лекарственная форма |
| ES2606227T3 (es) * | 2010-02-03 | 2017-03-23 | Grünenthal GmbH | Preparación de una composición farmacéutica en polvo mediante una extrusora |
| US20160176930A1 (en) | 2010-07-09 | 2016-06-23 | The Administrators Of The Tulane Educational Fund | Mu opioid receptor agonist analogs of the endomorphins |
| RU2604676C2 (ru) | 2010-09-02 | 2016-12-10 | Грюненталь Гмбх | Устойчивая к разрушению лекарственная форма, содержащая неорганическую соль |
| PE20131126A1 (es) | 2010-09-02 | 2013-10-21 | Gruenenthal Chemie | Forma de dosificacion resistente a alteracion que comprende un polimero anionico |
| DK2736497T3 (da) | 2011-07-29 | 2017-11-13 | Gruenenthal Gmbh | Stød-resistent tablet, der tilvejebringer en øjeblikkelig frigivelse af et lægemiddel. |
| CA2839123A1 (en) | 2011-07-29 | 2013-02-07 | Grunenthal Gmbh | Tamper-resistant tablet providing immediate drug release |
| US20130225697A1 (en) | 2012-02-28 | 2013-08-29 | Grunenthal Gmbh | Tamper-resistant dosage form comprising pharmacologically active compound and anionic polymer |
| WO2013156453A1 (en) | 2012-04-18 | 2013-10-24 | Grünenthal GmbH | Tamper resistant and dose-dumping resistant pharmaceutical dosage form |
| US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
| CN102964279B (zh) * | 2012-12-12 | 2014-05-07 | 中国药科大学 | 一类具有外周镇痛作用的κ阿片受体激动剂 |
| AR096438A1 (es) | 2013-05-29 | 2015-12-30 | Gruenenthal Gmbh | Forma de dosificación resistente al uso indebido con perfil de liberación bimodal, proceso |
| CA2907950A1 (en) | 2013-05-29 | 2014-12-04 | Grunenthal Gmbh | Tamper-resistant dosage form containing one or more particles |
| AU2014289187B2 (en) | 2013-07-12 | 2019-07-11 | Grunenthal Gmbh | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
| MX371372B (es) | 2013-11-26 | 2020-01-28 | Gruenenthal Gmbh | Preparacion de una composicion farmaceutica en polvo por medio de criomolienda. |
| EP3142646A1 (en) | 2014-05-12 | 2017-03-22 | Grünenthal GmbH | Tamper resistant immediate release capsule formulation comprising tapentadol |
| JP2017516789A (ja) | 2014-05-26 | 2017-06-22 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | エタノール過量放出に対して防護されている多粒子 |
| KR20170139158A (ko) | 2015-04-24 | 2017-12-18 | 그뤼넨탈 게엠베하 | 즉시 방출되고 용매 추출 방지된 변조 방지된 투여 형태 |
| CA2998259A1 (en) | 2015-09-10 | 2017-03-16 | Grunenthal Gmbh | Protecting oral overdose with abuse deterrent immediate release formulations |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE68926269T2 (de) * | 1988-06-30 | 1996-08-14 | Astra Ab | Dermorphin-Analoge, deren Herstellungsverfahren, pharmazeutische Zusammensetzungen und Methode zur therapeutischen Behandlung unter Verwendung der Analoge |
| IS4261A (is) | 1994-02-21 | 1995-08-22 | Astra Aktiebolag | Nýir peptíð-ópíóíðar til meðhöndlunar á verkjum og notkun þeirra |
-
1995
- 1995-11-07 SE SE9503924A patent/SE9503924D0/xx unknown
-
1996
- 1996-08-06 AR ARP960103900A patent/AR003475A1/es active IP Right Grant
- 1996-08-14 ES ES96927978T patent/ES2171224T3/es not_active Expired - Lifetime
- 1996-08-14 DK DK96927978T patent/DK0845003T3/da active
- 1996-08-14 WO PCT/SE1996/001011 patent/WO1997007130A1/en not_active Application Discontinuation
- 1996-08-14 BR BR9610248A patent/BR9610248A/pt unknown
- 1996-08-14 CA CA002229797A patent/CA2229797A1/en not_active Abandoned
- 1996-08-14 CN CN96197625A patent/CN1200127A/zh active Pending
- 1996-08-14 NZ NZ315809A patent/NZ315809A/xx unknown
- 1996-08-14 RU RU98104253/04A patent/RU2165432C2/ru active
- 1996-08-14 AU AU67600/96A patent/AU711862B2/en not_active Ceased
- 1996-08-14 EE EE9800048A patent/EE9800048A/xx unknown
- 1996-08-14 PL PL96325113A patent/PL325113A1/xx unknown
- 1996-08-14 US US08/718,585 patent/US6337319B1/en not_active Expired - Fee Related
- 1996-08-14 JP JP9509209A patent/JPH11512086A/ja active Pending
- 1996-08-14 IL IL12325896A patent/IL123258A/xx not_active IP Right Cessation
- 1996-08-14 AT AT96927978T patent/ATE210148T1/de not_active IP Right Cessation
- 1996-08-14 DE DE69617699T patent/DE69617699T2/de not_active Expired - Fee Related
- 1996-08-14 SK SK203-98A patent/SK282469B6/sk unknown
- 1996-08-14 HU HU9901209A patent/HUP9901209A3/hu unknown
- 1996-08-14 CZ CZ1998401A patent/CZ287299B6/cs not_active IP Right Cessation
- 1996-08-14 EP EP96927978A patent/EP0845003B1/en not_active Expired - Lifetime
- 1996-08-14 TR TR1998/00258T patent/TR199800258T1/xx unknown
- 1996-08-14 KR KR1019980701156A patent/KR19990037677A/ko not_active Application Discontinuation
- 1996-08-15 TW TW085109918A patent/TW424095B/zh not_active IP Right Cessation
-
1998
- 1998-02-04 IS IS4664A patent/IS4664A/is unknown
- 1998-02-11 NO NO980592A patent/NO980592D0/no not_active Application Discontinuation
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