ATE206716T1 - Cyclische wirkstoff-vorläufer verbindungen von peptiden und peptid-nukleicsäuren mit verbesserter metabolischer stabilität und zellmembran permeabilität - Google Patents
Cyclische wirkstoff-vorläufer verbindungen von peptiden und peptid-nukleicsäuren mit verbesserter metabolischer stabilität und zellmembran permeabilitätInfo
- Publication number
- ATE206716T1 ATE206716T1 AT96911444T AT96911444T ATE206716T1 AT E206716 T1 ATE206716 T1 AT E206716T1 AT 96911444 T AT96911444 T AT 96911444T AT 96911444 T AT96911444 T AT 96911444T AT E206716 T1 ATE206716 T1 AT E206716T1
- Authority
- AT
- Austria
- Prior art keywords
- cyclic
- cell membrane
- membrane permeability
- peptides
- peptide
- Prior art date
Links
- 210000000170 cell membrane Anatomy 0.000 title abstract 2
- 230000035699 permeability Effects 0.000 title abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 title abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 1
- 150000007513 acids Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 230000002503 metabolic effect Effects 0.000 title 1
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- UVQGLJHJZLVTQF-UHFFFAOYSA-N 3-(2-hydroxy-4,6-dimethylphenyl)-3-methylbutanoic acid Chemical compound CC1=CC(C)=C(C(C)(C)CC(O)=O)C(O)=C1 UVQGLJHJZLVTQF-UHFFFAOYSA-N 0.000 abstract 1
- 108091093037 Peptide nucleic acid Proteins 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
- C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
- C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
- C07K14/70—Enkephalins
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Toxicology (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Analytical Chemistry (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Anesthesiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/429,732 US5672584A (en) | 1995-04-25 | 1995-04-25 | Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane permeability |
| PCT/US1996/004180 WO1997039024A1 (en) | 1995-04-25 | 1996-04-08 | Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane permeability |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE206716T1 true ATE206716T1 (de) | 2001-10-15 |
Family
ID=23704505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT96911444T ATE206716T1 (de) | 1995-04-25 | 1996-04-08 | Cyclische wirkstoff-vorläufer verbindungen von peptiden und peptid-nukleicsäuren mit verbesserter metabolischer stabilität und zellmembran permeabilität |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US5672584A (de) |
| EP (1) | EP0830372B1 (de) |
| JP (1) | JPH11508275A (de) |
| AT (1) | ATE206716T1 (de) |
| AU (1) | AU702993B2 (de) |
| CA (1) | CA2219151A1 (de) |
| DE (1) | DE69615838T2 (de) |
| ES (1) | ES2165492T3 (de) |
| WO (1) | WO1997039024A1 (de) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6521737B1 (en) * | 1995-11-10 | 2003-02-18 | Elan Corporation, Plc | Peptides which enhance transport across tissues and methods of identifying and using the same |
| IE80466B1 (en) * | 1995-11-10 | 1998-07-29 | Elan Corp Plc | Peptides which enhance transport across tissues and methods of identifying and using the same |
| US6361938B1 (en) * | 1996-11-08 | 2002-03-26 | Elan Corporation, Plc | Peptides which enhance transport across tissues and methods of identifying and using the same |
| US6180095B1 (en) | 1997-12-17 | 2001-01-30 | Enzon, Inc. | Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents |
| JP4465109B2 (ja) | 1997-12-17 | 2010-05-19 | エンゾン ファーマシューティカルズ,インコーポレーテッド | アミノ及びヒドロキシル含有生物活性剤のポリマープロドラッグ |
| US6624142B2 (en) | 1997-12-30 | 2003-09-23 | Enzon, Inc. | Trimethyl lock based tetrapartate prodrugs |
| US5965119A (en) | 1997-12-30 | 1999-10-12 | Enzon, Inc. | Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents |
| US6030997A (en) * | 1998-01-21 | 2000-02-29 | Eilat; Eran | Acid labile prodrugs |
| EP2286792A1 (de) | 1999-02-26 | 2011-02-23 | Novartis Vaccines and Diagnostics, Inc. | Mikroemulsionen mit einer adsorbierenden Oberfläche, enthaltend eine Mikrotropfenemulsion |
| US7192713B1 (en) | 1999-05-18 | 2007-03-20 | President And Fellows Of Harvard College | Stabilized compounds having secondary structure motifs |
| US20020199218A1 (en) * | 1999-08-19 | 2002-12-26 | Daphne Goring | Proline-rich extensin-like receptor kinases |
| DE19942624A1 (de) * | 1999-08-28 | 2001-03-08 | Chemotopix Gmbh | Verfahren zur Herstellung von zyklischen Peptidomimetika |
| CA2364983A1 (en) * | 2000-12-13 | 2002-06-13 | John R. Coleman | Nucleic acid molecules and polypeptides for catabolism of abscisic acid |
| MXPA03007392A (es) * | 2001-02-20 | 2003-12-04 | Enzon Inc | Enlazantes polimericos ramificados terminalmente y conjugados polimericos que contienen los mismos. |
| WO2002087500A2 (en) * | 2001-04-27 | 2002-11-07 | Newbiotics, Inc. | Viral enzyme activated prototoxophores and use of same to treat viral infections |
| US7232924B2 (en) * | 2001-06-11 | 2007-06-19 | Xenoport, Inc. | Methods for synthesis of acyloxyalkyl derivatives of GABA analogs |
| US8048917B2 (en) | 2005-04-06 | 2011-11-01 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| MXPA03011566A (es) * | 2001-06-11 | 2004-10-28 | Xenoport Inc | Formas de dosificacion de profarmacos de analogos de gaba administrados oralmente que tienen toxicidad reducida. |
| US7186855B2 (en) | 2001-06-11 | 2007-03-06 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| US6818787B2 (en) * | 2001-06-11 | 2004-11-16 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| SI2332582T1 (sl) | 2002-06-19 | 2014-03-31 | Apeiron Biologics Ag | Aktivacija ACE2 za zdravljenje srčne, pljučne in ledvične bolezni in hipertenzije |
| WO2005044839A2 (en) * | 2003-11-05 | 2005-05-19 | Dana-Farber Cancer Institute, Inc. | Stabilized alpha helical peptides and uses thereof |
| WO2005047245A2 (en) * | 2003-11-14 | 2005-05-26 | Wisconsin Alumni Research Foundation | Fluorescence assays with improved blocking groups |
| EP1811986B1 (de) | 2004-11-04 | 2014-03-26 | XenoPort, Inc. | Orale darreichungsformen von gabapentin-prodrug mit verzögerter freisetzung |
| EP1910379B1 (de) * | 2005-07-28 | 2011-10-19 | Vertex Pharmaceuticals Incorporated | Caspase-hemmer-propharmaka |
| US8168592B2 (en) * | 2005-10-21 | 2012-05-01 | Amgen Inc. | CGRP peptide antagonists and conjugates |
| US20080261893A1 (en) * | 2006-02-24 | 2008-10-23 | Denise Barbut | Topical corneal analgesia using neurotensin receptor agonists and synergistic neurotensin combinations without delaying wound healing |
| US7531572B2 (en) * | 2006-07-28 | 2009-05-12 | Xenoport, Inc. | Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use |
| PL2118123T3 (pl) * | 2007-01-31 | 2016-06-30 | Dana Farber Cancer Inst Inc | Stabilizowane peptydy p53 i ich zastosowania |
| AU2008225100A1 (en) * | 2007-03-12 | 2008-09-18 | Mayo Foundation For Medical Education And Research | Topical corneal analgesia using neurotensin receptor agonists and synergistic neurotensin combinations without delaying wound healing |
| JP5631201B2 (ja) | 2007-03-28 | 2014-11-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | ステッチングされたポリペプチド |
| CN104474529A (zh) | 2008-02-08 | 2015-04-01 | 爱勒让治疗公司 | 治疗性的拟肽大环化合物 |
| US20110144303A1 (en) * | 2008-04-08 | 2011-06-16 | Aileron Therapeutics, Inc. | Biologically Active Peptidomimetic Macrocycles |
| CN104961795A (zh) | 2008-09-22 | 2015-10-07 | 爱勒让治疗公司 | 用于制备纯化的多肽组合物的方法 |
| AU2010204648B2 (en) | 2009-01-14 | 2016-09-01 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| JP2013505300A (ja) | 2009-09-22 | 2013-02-14 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| EP2768518A4 (de) | 2011-10-18 | 2015-05-27 | Aileron Therapeutics Inc | Peptidomimetische makrozyklen |
| CA2864120A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| RU2642299C2 (ru) | 2012-02-15 | 2018-01-24 | Эйлерон Терапьютикс, Инк. | P53 пептидомиметические макроциклы |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| KR101695792B1 (ko) * | 2014-09-04 | 2017-01-12 | 디오셀 주식회사 | 신규 세포막 투과 펩티드 및 생리활성 물질 전달체로서의 그의 용도 |
| CN107106642B (zh) | 2014-09-24 | 2021-02-26 | 艾瑞朗医疗公司 | 拟肽大环化合物及其制剂 |
| EP3197478A4 (de) | 2014-09-24 | 2018-05-30 | Aileron Therapeutics, Inc. | Peptidomimetische makrozyklen und verwendungen davon |
| JP2018516844A (ja) | 2015-03-20 | 2018-06-28 | エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. | ペプチド模倣大環状分子およびその使用 |
| US10059741B2 (en) | 2015-07-01 | 2018-08-28 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| EP3347372A4 (de) | 2015-09-10 | 2019-09-04 | Aileron Therapeutics, Inc. | Peptidomimetische makrocyclen als modulatoren von mcl-1 |
| CA3056681A1 (en) * | 2017-03-23 | 2018-09-27 | Trucode Gene Repair, Inc. | Peptide nucleic acid (pna) monomers with an orthogonally protected ester moiety |
| US20200255492A1 (en) | 2017-08-31 | 2020-08-13 | University Of Dundee | Leptin peptides and their use for treating neurological disorders |
| CN118184532A (zh) * | 2018-12-12 | 2024-06-14 | 中外制药株式会社 | 具有能形成分子内氢键的官能团的氨基酸、包含该氨基酸的肽化合物、及其制备方法 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4960790A (en) * | 1989-03-09 | 1990-10-02 | University Of Kansas | Derivatives of taxol, pharmaceutical compositions thereof and methods for the preparation thereof |
-
1995
- 1995-04-25 US US08/429,732 patent/US5672584A/en not_active Expired - Fee Related
-
1996
- 1996-04-08 ES ES96911444T patent/ES2165492T3/es not_active Expired - Lifetime
- 1996-04-08 AU AU54330/96A patent/AU702993B2/en not_active Ceased
- 1996-04-08 JP JP9534725A patent/JPH11508275A/ja not_active Ceased
- 1996-04-08 CA CA002219151A patent/CA2219151A1/en not_active Abandoned
- 1996-04-08 AT AT96911444T patent/ATE206716T1/de not_active IP Right Cessation
- 1996-04-08 EP EP96911444A patent/EP0830372B1/de not_active Expired - Lifetime
- 1996-04-08 WO PCT/US1996/004180 patent/WO1997039024A1/en not_active Ceased
- 1996-04-08 DE DE69615838T patent/DE69615838T2/de not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU5433096A (en) | 1997-11-07 |
| EP0830372B1 (de) | 2001-10-10 |
| CA2219151A1 (en) | 1997-10-23 |
| ES2165492T3 (es) | 2002-03-16 |
| JPH11508275A (ja) | 1999-07-21 |
| EP0830372A1 (de) | 1998-03-25 |
| WO1997039024A1 (en) | 1997-10-23 |
| AU702993B2 (en) | 1999-03-11 |
| US5672584A (en) | 1997-09-30 |
| DE69615838T2 (de) | 2002-04-25 |
| DE69615838D1 (de) | 2001-11-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |