MXPA03009586A - Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma. - Google Patents
Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma.Info
- Publication number
- MXPA03009586A MXPA03009586A MXPA03009586A MXPA03009586A MXPA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A
- Authority
- MX
- Mexico
- Prior art keywords
- group
- linear
- alkyl group
- carbon atoms
- alkyl
- Prior art date
Links
- 229940002612 prodrug Drugs 0.000 title abstract 2
- 239000000651 prodrug Substances 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 2
- 125000000539 amino acid group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invencion se refiere a un pro-farmaco que comprende un undecapeptido ciclico en donde la cadena del peptido del mismo comprende por lo menos un residuo de aminoacidos de la formula general (1) en donde el atomo de carbono Ca es uno de los enlaces en dicho ciclo undecapeptido; - substituyentes Y que representan individualmente un atomo de hidrogeno o forman un enlace juntos; - los substituyentes R1 y R3 representan independientemente un atomo de hidrogeno, un grupo aralquilo, un grupo alcarilo, un grupo heteroalquilo, un grupo heterociclico, un grupo alquilo heterociclico, un grupo heterociclico alquilo, o un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado, y que es opcionalmente sustituido por al menos uno de los grupos seleccionados entre -COOH, -CONHR8, -NHCO=NH(NH2), -NHC=NR8(NH2), -NH2, -NHR8, -NR82, -N+R83, -OH, -OPO(OR8)2, -OPO(OH)(OR8), -OPO(OH)2, -OSO(OR8)2, -OSO(OH)(OR8), -OSO(OH)2, y las diferentes sales producidas de los mismos, representando independientemente cada uno de los substituyentes R8 un grupo alquilo el cual es recto o ramificado que tiene de 1 a 6 atomos de carbono; - los substituyentes R2 y R4 representan independientemente un atomo de hidrogeno, un grupo alcarilo o un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado; - los substituyentes R5 y R6 representan individualmente un atomo de hidrogeno, un grupo aralquilo, un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado; y un substituyente R7 que representa un grupo alcarilo, un grupo heteroalquilo, un grupo heterociclico, un grupo alquilo heterociclico, un grupo heterociclico alquilo o un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH7202001 | 2001-04-20 | ||
| PCT/CH2002/000222 WO2002085928A2 (fr) | 2001-04-20 | 2002-04-22 | Cyclosporine modifiee utilisable en tant que pro-drogue et son utilisation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA03009586A true MXPA03009586A (es) | 2004-05-24 |
Family
ID=4531478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA03009586A MXPA03009586A (es) | 2001-04-20 | 2002-04-22 | Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma. |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US6995139B2 (es) |
| EP (1) | EP1379547B1 (es) |
| JP (1) | JP4588979B2 (es) |
| KR (1) | KR100932859B1 (es) |
| CN (1) | CN1507451A (es) |
| AT (1) | ATE313557T1 (es) |
| AU (1) | AU2002245996B8 (es) |
| BR (1) | BR0208923A (es) |
| CA (1) | CA2444278C (es) |
| DE (1) | DE60208180T2 (es) |
| ES (1) | ES2256450T3 (es) |
| IL (1) | IL158385A0 (es) |
| MX (1) | MXPA03009586A (es) |
| RU (1) | RU2290196C2 (es) |
| UA (1) | UA75136C2 (es) |
| WO (1) | WO2002085928A2 (es) |
| ZA (1) | ZA200307794B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8048917B2 (en) | 2005-04-06 | 2011-11-01 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| US7186855B2 (en) | 2001-06-11 | 2007-03-06 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| US7354574B2 (en) * | 2002-11-07 | 2008-04-08 | Advanced Ocular Systems Limited | Treatment of ocular disease |
| US7083803B2 (en) | 2003-09-19 | 2006-08-01 | Advanced Ocular Systems Limited | Ocular solutions |
| US7087237B2 (en) | 2003-09-19 | 2006-08-08 | Advanced Ocular Systems Limited | Ocular solutions |
| CA2571710A1 (en) | 2004-06-24 | 2006-11-02 | Nicholas Valiante | Small molecule immunopotentiators and assays for their detection |
| EP1904056B1 (en) | 2005-07-18 | 2009-04-29 | Minu, L.L.C. | Use of a macrolide to restore corneal sensation |
| 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 |
| US7531572B2 (en) | 2006-07-28 | 2009-05-12 | Xenoport, Inc. | Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use |
| US8394763B2 (en) | 2007-09-26 | 2013-03-12 | Oregon Health & Science University | Cyclic undecapeptides and derivatives as multiple sclerosis therapies |
| WO2009098533A1 (en) * | 2008-02-08 | 2009-08-13 | Debiopharm Sa | Non -immunosuppressive cyclosporin for the treatment of muscular dystrophy |
| GB0912584D0 (en) * | 2009-07-20 | 2009-08-26 | Ucl Business Plc | Cyclosporin conjugates |
| RU2630690C9 (ru) | 2010-12-15 | 2017-12-28 | КонтраВир Фармасьютикалз, Инк. | МОЛЕКУЛЫ АНАЛОГОВ ЦИКЛОСПОРИНА, МОДИФИЦИРОВАННЫЕ ПО 1 и 3 АМИНОКИСЛОТЕ |
| AR090964A1 (es) * | 2012-05-09 | 2014-12-17 | Novartis Ag | Proceso para la elaboracion de undecapeptidos ciclicos |
| CN113388002A (zh) * | 2021-06-10 | 2021-09-14 | 梯尔希（南京）药物研发有限公司 | 一种环孢菌素相关化合物的制备方法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4396542A (en) * | 1980-02-14 | 1983-08-02 | Sandoz Ltd. | Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production |
| ATE43335T1 (de) * | 1980-02-14 | 1989-06-15 | Sandoz Ag | Peptide die einen (1s,2r,3r)- oder (1r,2s,3s)-1nitrilo-1-carbonyl-3-methyl-2-oxyheptan oder hept-5-en-rest enthalten brauchbar in totaler synsthese von cyclosporinen, und verfahren zu ihrer herstellung. |
| US5169773A (en) * | 1984-10-04 | 1992-12-08 | Sandoz Ltd. | Monoclonal antibodies to cyclosporins |
| ATE43499T1 (de) * | 1984-10-10 | 1989-06-15 | Ile De France | Synergistische empfaengnisverhuetende mischung. |
| US4764503A (en) * | 1986-11-19 | 1988-08-16 | Sandoz Ltd. | Novel cyclosporins |
| DK0484281T4 (da) * | 1990-11-02 | 2001-02-05 | Novartis Ag | Cyclosporiner |
| US6187547B1 (en) * | 1993-09-08 | 2001-02-13 | Novartis Ag | Assay kit |
| GB9624038D0 (en) * | 1996-11-19 | 1997-01-08 | Sandoz Ltd | Organic compounds |
| US6017879A (en) * | 1998-04-03 | 2000-01-25 | B.M.R.A. Corporation B.V. | Template associated NPY Y2-receptor agonists |
| DE69928938T2 (de) | 1998-07-01 | 2006-08-17 | Debiopharm S.A. | Neues cyclosporin mit verbesserter wirkung |
| US6204257B1 (en) * | 1998-08-07 | 2001-03-20 | Universtiy Of Kansas | Water soluble prodrugs of hindered alcohols |
| DE60028936T2 (de) * | 1999-02-05 | 2007-01-11 | Debiopharm S.A. | Cyclosporin-derivate und verfahren zu deren herstellung |
| US6765019B1 (en) * | 1999-05-06 | 2004-07-20 | University Of Kentucky Research Foundation | Permeable, water soluble, non-irritating prodrugs of chemotherapeutic agents with oxaalkanoic acids |
| WO2001005819A1 (en) * | 1999-07-15 | 2001-01-25 | Kuhnil Pharm. Co., Ltd. | Novel water soluble-cyclosporine conjugated compounds |
| MXPA02001857A (es) * | 1999-08-24 | 2003-07-14 | Cellgate Inc | Composiciones y metodos para incrementar la entrega de drogas a traves y dentro de tejidos epiteliales. |
-
2002
- 2002-04-22 CA CA2444278A patent/CA2444278C/en not_active Expired - Fee Related
- 2002-04-22 UA UA20031110436A patent/UA75136C2/uk unknown
- 2002-04-22 JP JP2002583454A patent/JP4588979B2/ja not_active Expired - Fee Related
- 2002-04-22 MX MXPA03009586A patent/MXPA03009586A/es active IP Right Grant
- 2002-04-22 ES ES02713992T patent/ES2256450T3/es not_active Expired - Lifetime
- 2002-04-22 AT AT02713992T patent/ATE313557T1/de not_active IP Right Cessation
- 2002-04-22 WO PCT/CH2002/000222 patent/WO2002085928A2/fr active IP Right Grant
- 2002-04-22 BR BR0208923-8A patent/BR0208923A/pt active Search and Examination
- 2002-04-22 EP EP02713992A patent/EP1379547B1/fr not_active Expired - Lifetime
- 2002-04-22 CN CNA028094050A patent/CN1507451A/zh active Pending
- 2002-04-22 AU AU2002245996A patent/AU2002245996B8/en not_active Ceased
- 2002-04-22 RU RU2003133742/15A patent/RU2290196C2/ru not_active IP Right Cessation
- 2002-04-22 IL IL15838502A patent/IL158385A0/xx not_active IP Right Cessation
- 2002-04-22 US US10/474,396 patent/US6995139B2/en not_active Expired - Fee Related
- 2002-04-22 DE DE60208180T patent/DE60208180T2/de not_active Expired - Lifetime
-
2003
- 2003-10-06 ZA ZA200307794A patent/ZA200307794B/en unknown
- 2003-10-17 KR KR1020037013666A patent/KR100932859B1/ko not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| DE60208180T2 (de) | 2006-08-17 |
| CA2444278C (en) | 2011-11-22 |
| KR100932859B1 (ko) | 2009-12-23 |
| EP1379547A2 (fr) | 2004-01-14 |
| ZA200307794B (en) | 2004-07-19 |
| UA75136C2 (en) | 2006-03-15 |
| AU2002245996B2 (en) | 2005-06-30 |
| JP4588979B2 (ja) | 2010-12-01 |
| IL158385A0 (en) | 2004-05-12 |
| KR20030094357A (ko) | 2003-12-11 |
| RU2003133742A (ru) | 2005-03-20 |
| CA2444278A1 (en) | 2002-10-31 |
| AU2002245996B8 (en) | 2005-07-14 |
| US20040138108A1 (en) | 2004-07-15 |
| US6995139B2 (en) | 2006-02-07 |
| CN1507451A (zh) | 2004-06-23 |
| ES2256450T3 (es) | 2006-07-16 |
| ATE313557T1 (de) | 2006-01-15 |
| EP1379547B1 (fr) | 2005-12-21 |
| JP2004536051A (ja) | 2004-12-02 |
| RU2290196C2 (ru) | 2006-12-27 |
| DE60208180D1 (de) | 2006-01-26 |
| WO2002085928A2 (fr) | 2002-10-31 |
| BR0208923A (pt) | 2004-04-27 |
| WO2002085928A3 (fr) | 2003-04-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration | ||
| GB | Transfer or rights |