UY25327A1 - Péptidos opioides sintéticos que ejercen su acción agonista actuando selectivamente sobre receptores opioides kappa - Google Patents
Péptidos opioides sintéticos que ejercen su acción agonista actuando selectivamente sobre receptores opioides kappaInfo
- Publication number
- UY25327A1 UY25327A1 UY25327A UY25327A UY25327A1 UY 25327 A1 UY25327 A1 UY 25327A1 UY 25327 A UY25327 A UY 25327A UY 25327 A UY25327 A UY 25327A UY 25327 A1 UY25327 A1 UY 25327A1
- Authority
- UY
- Uruguay
- Prior art keywords
- phe
- opioid receptors
- synthetic
- peptides
- xaa1
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Veterinary Medicine (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Nutrition Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Péptidos que presentan alta selectividad por receptores opioides Kappa (KOR) y que tienen prolongada duración de acción periférica sin penetración significativa en el cerebro son creados en base a secuencias de cuatro isómeros D de porciones de aminoácidos que tiene un C-terminal los cuales son amidas mono o bi sustituidas. Un amidopéptido opioide sintético o una sal derivada del mismo farmacéuticamente aceptable caracterizado por que presenta afinidad por receptores opioides Kappa el cual es al menos 1000 veces más a fin que para los receptores opioide mu y que muestran una prolongada acción cuando es administrado in vivo, cuya fórmula es: H-Xaa1-Xaa2-Xaa3-Xaa4-Q donde Xaa1 es (A)D-Phe, (CalfaMe)D-Phe, D-Tyr, D-Tic o D-Ala (ciclopentil o tienil), con A siendo H, NO2, F, CL, o CH3; Xaa2 es (A')D-Phe, D-1Nal, D-2Nal, D-Tyr o D-trp; Xaa3 esD-Nle, (B)D-Leu, D-Hle, D-Met, D-Val, etc; Xaa4 es D-Har, D-Arg, D-Lys, D-Ily, D-Phe, etc; y Q es NR1R2, morfolinilo, tiomorfolinilo, piperacinilo, etc. Una composición farmacéutica que comprende una cantidad de antinociceptivo de un péptido sintetico y un transporte liquido o sólido farmacéuticamente aceptable; el cual es efectiva para lograr antonocicepción donde haya dolor visceral, artritis reumatoide, dolor crónico o agudo o para contrarrestar inestabilidad urinaria, incontinencia o cólicos digestivos, o para combatir IBD o enfermedades de autoinmunología.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/997,208 US5965701A (en) | 1997-12-23 | 1997-12-23 | Kappa receptor opioid peptides |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UY25327A1 true UY25327A1 (es) | 2000-12-29 |
Family
ID=25543752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY25327A UY25327A1 (es) | 1997-12-23 | 1998-12-23 | Péptidos opioides sintéticos que ejercen su acción agonista actuando selectivamente sobre receptores opioides kappa |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US5965701A (es) |
| EP (1) | EP1042359B1 (es) |
| JP (1) | JP4275852B2 (es) |
| KR (1) | KR100629548B1 (es) |
| CN (1) | CN1154655C (es) |
| AR (1) | AR014167A1 (es) |
| AT (1) | ATE301670T1 (es) |
| AU (1) | AU747806B2 (es) |
| BR (2) | BRPI9814499B8 (es) |
| CA (1) | CA2315878C (es) |
| CR (1) | CR5936A (es) |
| CZ (1) | CZ297281B6 (es) |
| DE (1) | DE69831176T2 (es) |
| DK (1) | DK1042359T3 (es) |
| EE (1) | EE04440B1 (es) |
| ES (1) | ES2247735T3 (es) |
| HK (1) | HK1029349A1 (es) |
| HR (1) | HRP20000415B1 (es) |
| HU (1) | HU227640B1 (es) |
| IL (3) | IL136742A0 (es) |
| MY (1) | MY117542A (es) |
| NO (1) | NO327080B1 (es) |
| NZ (1) | NZ505183A (es) |
| PL (1) | PL195842B1 (es) |
| PT (1) | PT1042359E (es) |
| RU (1) | RU2217437C2 (es) |
| SK (1) | SK286135B6 (es) |
| TR (1) | TR200001985T2 (es) |
| TW (1) | TW580502B (es) |
| UA (1) | UA68366C2 (es) |
| UY (1) | UY25327A1 (es) |
| WO (1) | WO1999032510A1 (es) |
| ZA (1) | ZA9811801B (es) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9006175B2 (en) | 1999-06-29 | 2015-04-14 | Mannkind Corporation | Potentiation of glucose elimination |
| WO2001036006A1 (en) * | 1999-11-19 | 2001-05-25 | Palatin Technologies, Inc. | Opioid metallopeptide compositions and methods |
| DE10116978A1 (de) * | 2001-04-05 | 2002-10-10 | Merck Patent Gmbh | Kappa-Opiatagonisten für die Behandlung von Erkrankungen der Blase |
| EP1402899A4 (en) * | 2001-05-08 | 2009-03-11 | Toray Industries | MEANS FOR THE TREATMENT OF SEPSIS |
| WO2003080149A2 (en) | 2002-03-20 | 2003-10-02 | Mannkind Corporation | Inhalation apparatus |
| DE602005024413D1 (de) | 2004-08-20 | 2010-12-09 | Mannkind Corp | Katalyse der diketopiperazinsynthese |
| ES2540886T3 (es) | 2004-08-23 | 2015-07-14 | Mannkind Corporation | Sales de dicetopiperazina para la administración de fármacos |
| KR101557502B1 (ko) | 2005-09-14 | 2015-10-06 | 맨카인드 코포레이션 | 결정질 미립자 표면에 대한 활성제의 친화력의 증가를기반으로 하는 약물 제제의 방법 |
| AU2007216966C1 (en) | 2006-02-22 | 2014-03-20 | Mannkind Corporation | A method for improving the pharmaceutic properties of microparticles comprising diketopiperazine and an active agent |
| US20100029575A1 (en) * | 2006-05-26 | 2010-02-04 | Jean-Louis Junien | N-Oxides of Kappa Receptor Peptides |
| EP2040733A2 (en) * | 2006-05-26 | 2009-04-01 | Cara Therapeutics, Inc. | Method for elevating prolactin in mammals |
| 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 |
| US8236766B2 (en) * | 2006-11-10 | 2012-08-07 | Cara Therapeutics, Inc. | Uses of synthetic peptide amides |
| NZ577107A (en) * | 2006-11-10 | 2012-01-12 | Cara Therapeutics Inc | Synthetic peptide amide ligands of the kappa opiod receptor |
| US7713937B2 (en) * | 2006-11-10 | 2010-05-11 | Cara Therapeutics, Inc. | Synthetic peptide amides and dimeric forms thereof |
| WO2008077194A1 (en) * | 2006-12-22 | 2008-07-03 | Xenome Ltd | Receptor agonists |
| US8485180B2 (en) | 2008-06-13 | 2013-07-16 | Mannkind Corporation | Dry powder drug delivery system |
| PL2293833T3 (pl) | 2008-06-13 | 2016-08-31 | Mannkind Corp | Inhalator proszkowy i układ do dostarczania leku |
| EP2609954B1 (en) | 2008-06-20 | 2021-12-29 | MannKind Corporation | An interactive apparatus for real-time profiling of inhalation efforts |
| TWI532497B (zh) | 2008-08-11 | 2016-05-11 | 曼凱公司 | 超快起作用胰島素之用途 |
| US8314106B2 (en) | 2008-12-29 | 2012-11-20 | Mannkind Corporation | Substituted diketopiperazine analogs for use as drug delivery agents |
| EP2405963B1 (en) | 2009-03-11 | 2013-11-06 | MannKind Corporation | Apparatus, system and method for measuring resistance of an inhaler |
| KR20180079458A (ko) | 2009-06-12 | 2018-07-10 | 맨카인드 코포레이션 | 한정된 비표면적을 갖는 디케토피페라진 마이크로입자 |
| US9016147B2 (en) | 2009-11-03 | 2015-04-28 | Mannkind Corporation | Apparatus and method for simulating inhalation efforts |
| CA2801936C (en) | 2010-06-21 | 2021-06-01 | Mannkind Corporation | Dry powder drug delivery system and methods |
| EP2694402B1 (en) | 2011-04-01 | 2017-03-22 | MannKind Corporation | Blister package for pharmaceutical cartridges |
| WO2012174472A1 (en) | 2011-06-17 | 2012-12-20 | Mannkind Corporation | High capacity diketopiperazine microparticles |
| EP2776053A1 (en) | 2011-10-24 | 2014-09-17 | MannKind Corporation | Methods and compositions for treating pain |
| AU2013289957B2 (en) | 2012-07-12 | 2017-02-23 | Mannkind Corporation | Dry powder drug delivery systems and methods |
| EP2911690A1 (en) | 2012-10-26 | 2015-09-02 | MannKind Corporation | Inhalable influenza vaccine compositions and methods |
| KR102499439B1 (ko) | 2013-03-15 | 2023-02-13 | 맨카인드 코포레이션 | 미세결정성 디케토피페라진 조성물 및 방법 |
| MX2020009878A (es) | 2013-07-18 | 2022-07-27 | Mannkind Corp | Composiciones farmaceuticas en polvo seco estables al calor y metodos. |
| JP2016530930A (ja) | 2013-08-05 | 2016-10-06 | マンカインド コーポレイション | 通気装置及び方法 |
| US10307464B2 (en) | 2014-03-28 | 2019-06-04 | Mannkind Corporation | Use of ultrarapid acting insulin |
| EP3162810B1 (en) * | 2014-06-26 | 2019-02-13 | Maruishi Pharmaceutical Co., Ltd. | Method for producing synthetic pentapeptide |
| US10561806B2 (en) | 2014-10-02 | 2020-02-18 | Mannkind Corporation | Mouthpiece cover for an inhaler |
| JP6651546B2 (ja) * | 2015-05-11 | 2020-02-19 | カディラ・ヘルスケア・リミテッド | カッパ（κ）オピオイド受容体（ＫＯＲ）アゴニストとしての新規の短鎖ペプチド |
| CN107098876B (zh) * | 2016-02-23 | 2021-04-06 | 江苏恒瑞医药股份有限公司 | 苯基丙酰胺类衍生物、其制备方法及其在医药上的应用 |
| EP3521301B1 (en) * | 2016-09-27 | 2024-03-06 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Polyamide compound and use thereof |
| KR102375543B1 (ko) * | 2017-07-21 | 2022-03-16 | 스촨 하이스코 파마수티컬 씨오., 엘티디 | 펩티드 아미드류 화합물 및 이의 제조 방법과 의약에서의 용도 |
| AU2018380170A1 (en) | 2017-12-06 | 2020-06-11 | Jiangsu Hengrui Medicine Co., Ltd. | Salt of phenylpropionamide derivative and preparation method therefor |
| CN111148526B (zh) | 2018-05-16 | 2023-03-10 | 江苏恒瑞医药股份有限公司 | 一种kor受体激动剂药物组合物 |
| CN114127086B (zh) * | 2019-07-25 | 2023-10-20 | 四川海思科制药有限公司 | 氘代肽酰胺类化合物及其制备方法和在医药上的用途 |
| CN114127085B (zh) * | 2019-07-25 | 2024-08-13 | 西藏海思科制药有限公司 | 一种肽酰胺盐及其制备方法和在医药上的用途 |
| US20210040150A1 (en) * | 2019-08-07 | 2021-02-11 | Humanwell Pharmaceutical US | Kappa opioid receptor peptide amide agonists |
| AU2020454871A1 (en) | 2020-06-25 | 2023-01-19 | Humanwell Pharmaceutical US | Peptides for treatment of medical disorders |
| WO2023278843A2 (en) | 2021-07-02 | 2023-01-05 | Acer Therapeutics, Inc. | Solid forms of osanetant |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2013689B (en) * | 1977-12-15 | 1982-03-24 | Reckitt & Colmann Prod Ltd | Compounds |
| GB8801304D0 (en) * | 1988-01-21 | 1988-02-17 | Ici Plc | Diamine compounds |
| US5367053A (en) * | 1993-05-19 | 1994-11-22 | Houghten Pharmaceuticals, Inc. | Opioid peptide inhibitors |
| US5610271A (en) * | 1995-06-07 | 1997-03-11 | Torrey Pines Institute For Molecular Studies | Kappa receptor selective opioid peptides |
-
1997
- 1997-12-23 US US08/997,208 patent/US5965701A/en not_active Expired - Lifetime
-
1998
- 1998-12-22 CA CA2315878A patent/CA2315878C/en not_active Expired - Lifetime
- 1998-12-22 MY MYPI98005818A patent/MY117542A/en unknown
- 1998-12-22 UA UA2000063810A patent/UA68366C2/uk unknown
- 1998-12-22 AT AT98964224T patent/ATE301670T1/de active
- 1998-12-22 EP EP98964224A patent/EP1042359B1/en not_active Expired - Lifetime
- 1998-12-22 BR BRPI9814499A patent/BRPI9814499B8/pt unknown
- 1998-12-22 ES ES98964224T patent/ES2247735T3/es not_active Expired - Lifetime
- 1998-12-22 KR KR1020007006936A patent/KR100629548B1/ko not_active IP Right Cessation
- 1998-12-22 BR BRPI9814499-5A patent/BR9814499B1/pt not_active IP Right Cessation
- 1998-12-22 HU HU0100626A patent/HU227640B1/hu not_active IP Right Cessation
- 1998-12-22 PT PT98964224T patent/PT1042359E/pt unknown
- 1998-12-22 IL IL13674298A patent/IL136742A0/xx active IP Right Grant
- 1998-12-22 CZ CZ20002382A patent/CZ297281B6/cs not_active IP Right Cessation
- 1998-12-22 CR CR5936A patent/CR5936A/es unknown
- 1998-12-22 TR TR2000/01985T patent/TR200001985T2/xx unknown
- 1998-12-22 ZA ZA9811801A patent/ZA9811801B/xx unknown
- 1998-12-22 JP JP2000525447A patent/JP4275852B2/ja not_active Expired - Lifetime
- 1998-12-22 CN CNB98812582XA patent/CN1154655C/zh not_active Expired - Lifetime
- 1998-12-22 AU AU19402/99A patent/AU747806B2/en not_active Ceased
- 1998-12-22 EE EEP200000370A patent/EE04440B1/xx not_active IP Right Cessation
- 1998-12-22 WO PCT/US1998/027282 patent/WO1999032510A1/en active IP Right Grant
- 1998-12-22 DK DK98964224T patent/DK1042359T3/da active
- 1998-12-22 DE DE69831176T patent/DE69831176T2/de not_active Expired - Lifetime
- 1998-12-22 NZ NZ505183A patent/NZ505183A/en not_active IP Right Cessation
- 1998-12-22 PL PL98341308A patent/PL195842B1/pl not_active IP Right Cessation
- 1998-12-22 SK SK960-2000A patent/SK286135B6/sk not_active IP Right Cessation
- 1998-12-22 RU RU2000119773/04A patent/RU2217437C2/ru active
- 1998-12-23 AR ARP980106652A patent/AR014167A1/es active IP Right Grant
- 1998-12-23 UY UY25327A patent/UY25327A1/es unknown
-
1999
- 1999-02-10 TW TW087121390A patent/TW580502B/zh not_active IP Right Cessation
-
2000
- 2000-06-12 IL IL136742A patent/IL136742A/en not_active IP Right Cessation
- 2000-06-20 HR HR20000415A patent/HRP20000415B1/xx not_active IP Right Cessation
- 2000-06-21 NO NO20003245A patent/NO327080B1/no not_active IP Right Cessation
- 2000-11-28 HK HK00107625A patent/HK1029349A1/xx not_active IP Right Cessation
-
2006
- 2006-10-05 IL IL178471A patent/IL178471A0/en unknown
Also Published As
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