ECSP045059A - Sintesis de analogos de ciclosporina - Google Patents
Sintesis de analogos de ciclosporinaInfo
- Publication number
- ECSP045059A ECSP045059A EC2004005059A ECSP045059A ECSP045059A EC SP045059 A ECSP045059 A EC SP045059A EC 2004005059 A EC2004005059 A EC 2004005059A EC SP045059 A ECSP045059 A EC SP045059A EC SP045059 A ECSP045059 A EC SP045059A
- Authority
- EC
- Ecuador
- Prior art keywords
- isomers
- cyclosporin
- stereo
- isatx247
- mixtures
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
- C07K7/645—Cyclosporins; Related peptides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
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- 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
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Dispersion Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
Abstract
El invento está dirigido hacia mezclas isómeras de análogos de ciclosporina que son estructuralmente similares a la ciclosporina A. Las mezclas poseen eficacia afianzada y reducida toxicidad con respecto a los isómeros individuales y por sobre ciclosporinas que ocurren naturalmente y derivados de ciclosporina actualmente conocidos. Las presentaciones del presente invento están dirigidas hacia cis y trans-isómeros de análogos de ciclosporina A que se han denominado ISATx247, y sus derivados. Las mezclas de isómeros ISATx247 exhiben una combinación de mayor potencia y menor toxicidad con respecto a ciclosporinas que ocurren naturalmente y que se conocen actualmente. Los isómeros ISATx247 y derivados alcalinados, arilados y deuterados se sintetizan mediante vías estéreo-selectivas en las que las condiciones particulares de una reacción determinan el grado de estéreo-selectividad. Las vías estéreo-selectivas podrán utilizar una reacción Wittig, o un reactivo órgano-metálico que comprende elementos inorgánicos tales como boro, silicón, titanio, y litio. La tasa de isómeros en una mezcla podrá variar de entre alrededor de 10 a 90 por ciento según peso del isómero (E) hasta alrededor de 90 a 10 por ciento según peso del isómero (Z), de acuerdo al peso total de la mezcla.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34620101P | 2001-10-19 | 2001-10-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP045059A true ECSP045059A (es) | 2004-07-23 |
Family
ID=23358378
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2004005061A ECSP045061A (es) | 2001-10-19 | 2004-04-14 | Mezclas analogas de ciclosporina y su uso como agentes inmunomoduladores |
| EC2004005059A ECSP045059A (es) | 2001-10-19 | 2004-04-14 | Sintesis de analogos de ciclosporina |
| EC2004005060A ECSP045060A (es) | 2001-10-19 | 2004-04-14 | Nuevas formulaciones analogas de ciclosporina |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2004005061A ECSP045061A (es) | 2001-10-19 | 2004-04-14 | Mezclas analogas de ciclosporina y su uso como agentes inmunomoduladores |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2004005060A ECSP045060A (es) | 2001-10-19 | 2004-04-14 | Nuevas formulaciones analogas de ciclosporina |
Country Status (38)
| Country | Link |
|---|---|
| US (2) | US20110092669A1 (es) |
| EP (2) | EP1436322B1 (es) |
| JP (4) | JP2005511538A (es) |
| KR (1) | KR100992850B1 (es) |
| CN (1) | CN100344648C (es) |
| AR (1) | AR036853A1 (es) |
| AT (1) | ATE401339T1 (es) |
| AU (1) | AU2002331510B2 (es) |
| BE (1) | BE2022C547I2 (es) |
| BR (1) | BR0213659A (es) |
| CA (2) | CA2727642C (es) |
| CO (1) | CO5570682A2 (es) |
| CY (2) | CY1108410T1 (es) |
| DE (1) | DE60227686D1 (es) |
| DK (1) | DK1436322T3 (es) |
| EC (3) | ECSP045061A (es) |
| ES (1) | ES2310604T3 (es) |
| FI (1) | FIC20220041I1 (es) |
| FR (1) | FR22C1051I2 (es) |
| HR (1) | HRP20040353B1 (es) |
| IL (2) | IL160762A0 (es) |
| LT (1) | LTC1436322I2 (es) |
| MA (1) | MA26337A1 (es) |
| ME (1) | ME00487B (es) |
| MX (1) | MXPA04003624A (es) |
| MY (1) | MY187182A (es) |
| NL (1) | NL301200I2 (es) |
| NO (2) | NO331745B1 (es) |
| NZ (1) | NZ531945A (es) |
| PL (1) | PL210697B1 (es) |
| PT (1) | PT1436322E (es) |
| PY (2) | PY0225477A (es) |
| RU (1) | RU2337106C2 (es) |
| SI (1) | SI1436322T1 (es) |
| TN (1) | TNSN04069A1 (es) |
| UY (1) | UY27502A1 (es) |
| WO (1) | WO2003033527A2 (es) |
| ZA (1) | ZA200402270B (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003033526A2 (en) | 2001-10-19 | 2003-04-24 | Isotechnika Inc. | Synthesis of cyclosporin analogs |
| ES2310604T3 (es) * | 2001-10-19 | 2009-01-16 | Isotechnika, Inc. | Mezclas de analogos de ciclosporinas y su uso como agentes inmunomoduladores. |
| JP2006524232A (ja) | 2003-03-17 | 2006-10-26 | アルバニー モレキュラー リサーチ インコーポレーティッド | 新規サイクロスポリン |
| TW200505946A (en) * | 2003-04-08 | 2005-02-16 | Hoffmann La Roche | Process for preparation of cyclosporin a analog |
| EP1804823A4 (en) | 2004-09-29 | 2010-06-09 | Amr Technology Inc | NEW CYCLOSPORIN ANALOGUE AND ITS PHARMACEUTICAL APPLICATIONS |
| JP2008514701A (ja) | 2004-09-29 | 2008-05-08 | エーエムアール テクノロジー インコーポレイテッド | シクロスポリンアルキン類似体およびそれらの薬学的使用 |
| US7361636B2 (en) | 2004-10-06 | 2008-04-22 | Amr Technology, Inc. | Cyclosporin alkynes and their utility as pharmaceutical agents |
| CA2592343A1 (en) * | 2004-12-17 | 2006-06-22 | Isotechnika Inc. | Metabolites of cyclosporin analogs |
| CA2623898C (en) * | 2005-10-26 | 2013-12-24 | Astellas Pharma Inc. | New cyclic peptide compounds |
| US7696165B2 (en) | 2006-03-28 | 2010-04-13 | Albany Molecular Research, Inc. | Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders |
| US7696166B2 (en) | 2006-03-28 | 2010-04-13 | Albany Molecular Research, Inc. | Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders |
| ES2396170T3 (es) * | 2007-05-02 | 2013-02-19 | Astellas Pharma Inc. | Nuevos compuestos péptídicos ciclicos |
| US8435544B2 (en) | 2007-10-08 | 2013-05-07 | Lux Biosciences, Inc. | Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors |
| RU2361604C1 (ru) * | 2007-10-29 | 2009-07-20 | Федеральное агентство по высокотехнологичной медицинской помощи Федеральное государственное учреждение "Уральский научно-исследовательский институт дерматовенерологии и иммунопатологии" (ФГУ УрНИИДВиИ Росмедтехнологий) | Способ лечения атопического дерматита |
| WO2010144194A1 (en) | 2009-06-09 | 2010-12-16 | Lux Biosciences, Inc. | Topical drug delivery systems for ophthalmic use |
| GB0912584D0 (en) * | 2009-07-20 | 2009-08-26 | Ucl Business Plc | Cyclosporin conjugates |
| JP6144627B2 (ja) | 2010-12-15 | 2017-06-07 | コントラヴィア ファーマシューティカルズ、インク． | アミノ酸１および３で修飾されたシクロスポリン類似体分子 |
| GB201222455D0 (en) | 2012-12-13 | 2013-01-30 | Perioc Ltd | Novel pharmaceutical formulations and their use in the treatment of periodontaldisease |
| JP2020510249A (ja) * | 2016-11-30 | 2020-04-02 | シュレーディンガー インコーポレイテッドＳｃｈｒｏｄｉｎｇｅｒ，Ｉｎｃ． | 化学の遷移状態を計算するためのグラフィカルユーザインタフェース |
| EP3551034A1 (en) | 2016-12-07 | 2019-10-16 | Progenity, Inc. | Gastrointestinal tract detection methods, devices and systems |
| WO2018106928A1 (en) | 2016-12-08 | 2018-06-14 | Contravir Pharmaceuticals, Inc. | Treatment and prevention of hbv diseases by cyclosporine analogue molecules modified at amino acides 1 and 3 |
| WO2018112255A1 (en) | 2016-12-14 | 2018-06-21 | Progenity Inc. | Treatment of a disease of the gastrointestinal tract with an immunosuppressant |
| US10286036B2 (en) * | 2017-05-12 | 2019-05-14 | Aurinia Pharmaceuticals Inc. | Protocol for treatment of lupus nephritis |
| US20190224275A1 (en) | 2017-05-12 | 2019-07-25 | Aurinia Pharmaceuticals Inc. | Protocol for treatment of lupus nephritis |
| WO2019246312A1 (en) | 2018-06-20 | 2019-12-26 | Progenity, Inc. | Treatment of a disease of the gastrointestinal tract with an immunomodulator |
| IL296586B1 (en) * | 2020-03-26 | 2026-04-01 | Farsight Medical Tech Shanghai Co Ltd | Cyclophilin inhibitors and their uses |
| EP4201952A1 (en) | 2021-12-21 | 2023-06-28 | Curia Spain, S.A.U. | Process for the controlled synthesis of voclosporin |
| EP4584279A1 (en) * | 2022-09-09 | 2025-07-16 | Dr. Reddy's Laboratories Limited | Improved process for the preparation of voclosporin |
| IT202300001116A1 (it) * | 2023-01-25 | 2024-07-25 | Indena Spa | Processo per la preparazione di un intermedio utile per la sintesi di voclosporina |
| IT202300001056A1 (it) * | 2023-01-25 | 2024-07-25 | Procos Spa | Nuovo processo per la preparazione di voclosporina amorfa |
| WO2025119925A1 (en) | 2023-12-05 | 2025-06-12 | Medichem, S.A. | Process for preparing voclosporin |
| IT202300028041A1 (it) * | 2023-12-27 | 2025-06-27 | Indena Spa | Processo per la preparazione di voclosporina |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4278545A (en) * | 1979-09-12 | 1981-07-14 | The Bendix Corporation | Apparatus for separating solids and liquid components |
| CH670644A5 (es) * | 1986-12-18 | 1989-06-30 | Lonza Ag | |
| US5162540A (en) * | 1986-12-18 | 1992-11-10 | Lonza Ltd. | Process for the production of (+) biotin |
| ES2059558T3 (es) * | 1987-06-17 | 1994-11-16 | Sandoz Ag | Ciclosporins y su uso como productos farmaceuticos. |
| US5972630A (en) * | 1991-08-19 | 1999-10-26 | Dade Behring Marburg Gmbh | Homogeneous immunoassays using enzyme inhibitors |
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