BR0208923A - Ciclosporina modificada que pode ser usada como um pró-fármaco e uso dela - Google Patents
Ciclosporina modificada que pode ser usada como um pró-fármaco e uso delaInfo
- Publication number
- BR0208923A BR0208923A BR0208923-8A BR0208923A BR0208923A BR 0208923 A BR0208923 A BR 0208923A BR 0208923 A BR0208923 A BR 0208923A BR 0208923 A BR0208923 A BR 0208923A
- Authority
- BR
- Brazil
- Prior art keywords
- group
- branched
- straight
- carbon atoms
- alkyl
- Prior art date
Links
- 229940002612 prodrug Drugs 0.000 title abstract 3
- 239000000651 prodrug Substances 0.000 title abstract 3
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical class CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 title abstract 2
- 229940064638 modified cyclosporine Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000004432 carbon atom Chemical group C* 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004122 cyclic 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
- 125000005343 heterocyclic alkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl 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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
"CICLOSPORINA MODIFICADA QUE PODE SER USADA COMO UM PRó-FáRMACO E USO DELA". A invenção se refere a um pró-fármaco compreendendo um undecapeptídeo cíclico no qual a cadeia peptídica dele compreende pelo menos um resíduo amino ácido da fórmula (1) em que o átomo de carbono C^ a^ é uma das ligações no referido undecapeptídeo cíclico; - substituintes Y individualmente representam um átomo de hidrogênio ou foram juntos uma ligação; substituintes R^ 1^ e R^ 3^ independentemente representam um átomo de hidrogênio, um grupo aralquil, um grupo alquaril, um grupo heteroalquil, um grupo heterocíclico, um grupo alquil heterocíclico, um grupo heterocíclico alquil ou um grupo alquil tendo de 1 a 6 átomos de carbono que é linear ou ramificado, e que é opcionalmente substituído por pelo menos um dos grupos escolhidos dentre -COOH,-CONHR^ 8^, -NHCO=NH(NH~ 2~),-NHC=NR^ 8^ (NH~ 2~), -NH~ 2~, -NHR^ 8^, -NR^ 8^~ 2~,-N ^ +^R^ 8^~ 3~, -OH, -OPO(OR^ 8^)~ 2~, -OPO(OH)(OR^ 8^), -OPO(OH)~ 2~, -OSO(OR^ 8^)~ 2~, -OSO(OH)(OR^ 8^), -OSO(OH)~ 2~, e os diferentes sais produzidos deles, cada um dos substituintes R^ 8^ representando, independentemente um grupo alquil que é linear ou ramificado tendo de 1 to 6 átomos de carbono; - os substituintes R^ 2^ e R^ 4^ representam, independentemente, um átomo de hidrogênio, um grupo alquaril, ou grupo alquil tendo de 1 a 6 átomos de carbono que é linear ou ramificado; - os substituintes R^ 5^ and R^ 6^ representam, independentemente, um átomo de hidrogênio, um grupo aralquil, ou um grupo alquil tendo de 1 to 6 átomos de carbono que é linear ou ramificado; e o substituinte R^ 7^ representa um alquaril, um grupo heteroalquil, um grupo heterocíclico, um grupo alquilheterocíclico, um grupo heterocicloalquil ou grupo alquil tendo de 1 to 6 átomos de carbono, que é linear ou 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 |
|---|---|
| BR0208923A true BR0208923A (pt) | 2004-04-27 |
Family
ID=4531478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0208923-8A BR0208923A (pt) | 2001-04-20 | 2002-04-22 | Ciclosporina modificada que pode ser usada como um pró-fármaco e uso dela |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US6995139B2 (pt) |
| EP (1) | EP1379547B1 (pt) |
| JP (1) | JP4588979B2 (pt) |
| KR (1) | KR100932859B1 (pt) |
| CN (1) | CN1507451A (pt) |
| AT (1) | ATE313557T1 (pt) |
| AU (1) | AU2002245996B8 (pt) |
| BR (1) | BR0208923A (pt) |
| CA (1) | CA2444278C (pt) |
| DE (1) | DE60208180T2 (pt) |
| ES (1) | ES2256450T3 (pt) |
| IL (1) | IL158385A0 (pt) |
| MX (1) | MXPA03009586A (pt) |
| RU (1) | RU2290196C2 (pt) |
| UA (1) | UA75136C2 (pt) |
| WO (1) | WO2002085928A2 (pt) |
| ZA (1) | ZA200307794B (pt) |
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 |
| EP1768662A2 (en) | 2004-06-24 | 2007-04-04 | Novartis Vaccines and Diagnostics, Inc. | Small molecule immunopotentiators and assays for their detection |
| AU2006270041B2 (en) | 2005-07-18 | 2011-08-18 | Minu, Llc | Enhanced ocular neuroprotection/neurostimulation |
| 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 |
| US7696165B2 (en) | 2006-03-28 | 2010-04-13 | Albany Molecular Research, Inc. | Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders |
| TW200820963A (en) * | 2006-07-28 | 2008-05-16 | 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 |
| DK2651965T3 (en) | 2010-12-15 | 2019-02-18 | Contravir Pharmaceuticals Inc | CYCLOSPORIN ANALOGUAL MODULES MODIFIED BY AMINO ACID 1 AND 3 |
| 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 |
| EP0034567B1 (en) * | 1980-02-14 | 1984-11-07 | Sandoz Ag | A method for the total synthesis of cyclosporins and novel cyclosporins |
| US5169773A (en) * | 1984-10-04 | 1992-12-08 | Sandoz Ltd. | Monoclonal antibodies to cyclosporins |
| DE3478398D1 (en) * | 1984-10-10 | 1989-07-06 | Ile De France | Synergistic contraceptive mixture |
| US4764503A (en) * | 1986-11-19 | 1988-08-16 | Sandoz Ltd. | Novel cyclosporins |
| FI111730B (fi) * | 1990-11-02 | 2003-09-15 | Novartis Ag | Menetelmä ei-immunosuppressiivisen syklosporiinin valmistamiseksi |
| 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 |
| EP1150999B1 (fr) * | 1999-02-05 | 2006-06-21 | Debiopharm S.A. | Derives de cyclosporine et procede de preparation desdits derives |
| 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 |
| US6593292B1 (en) * | 1999-08-24 | 2003-07-15 | Cellgate, Inc. | Compositions and methods for enhancing drug delivery across and into epithelial tissues |
-
2002
- 2002-04-22 IL IL15838502A patent/IL158385A0/xx not_active IP Right Cessation
- 2002-04-22 AT AT02713992T patent/ATE313557T1/de not_active IP Right Cessation
- 2002-04-22 RU RU2003133742/15A patent/RU2290196C2/ru not_active IP Right Cessation
- 2002-04-22 UA UA20031110436A patent/UA75136C2/uk unknown
- 2002-04-22 CN CNA028094050A patent/CN1507451A/zh active Pending
- 2002-04-22 BR BR0208923-8A patent/BR0208923A/pt active Search and Examination
- 2002-04-22 DE DE60208180T patent/DE60208180T2/de not_active Expired - Lifetime
- 2002-04-22 AU AU2002245996A patent/AU2002245996B8/en not_active Ceased
- 2002-04-22 WO PCT/CH2002/000222 patent/WO2002085928A2/fr active IP Right Grant
- 2002-04-22 JP JP2002583454A patent/JP4588979B2/ja not_active Expired - Fee Related
- 2002-04-22 CA CA2444278A patent/CA2444278C/en not_active Expired - Fee Related
- 2002-04-22 ES ES02713992T patent/ES2256450T3/es not_active Expired - Lifetime
- 2002-04-22 EP EP02713992A patent/EP1379547B1/fr not_active Expired - Lifetime
- 2002-04-22 MX MXPA03009586A patent/MXPA03009586A/es active IP Right Grant
- 2002-04-22 US US10/474,396 patent/US6995139B2/en not_active Expired - Fee Related
-
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 |
|---|---|
| ES2256450T3 (es) | 2006-07-16 |
| CN1507451A (zh) | 2004-06-23 |
| US20040138108A1 (en) | 2004-07-15 |
| CA2444278A1 (en) | 2002-10-31 |
| RU2290196C2 (ru) | 2006-12-27 |
| KR100932859B1 (ko) | 2009-12-23 |
| AU2002245996B8 (en) | 2005-07-14 |
| ZA200307794B (en) | 2004-07-19 |
| EP1379547A2 (fr) | 2004-01-14 |
| WO2002085928A3 (fr) | 2003-04-17 |
| MXPA03009586A (es) | 2004-05-24 |
| US6995139B2 (en) | 2006-02-07 |
| DE60208180D1 (de) | 2006-01-26 |
| EP1379547B1 (fr) | 2005-12-21 |
| UA75136C2 (en) | 2006-03-15 |
| RU2003133742A (ru) | 2005-03-20 |
| IL158385A0 (en) | 2004-05-12 |
| ATE313557T1 (de) | 2006-01-15 |
| JP4588979B2 (ja) | 2010-12-01 |
| AU2002245996B2 (en) | 2005-06-30 |
| DE60208180T2 (de) | 2006-08-17 |
| WO2002085928A2 (fr) | 2002-10-31 |
| CA2444278C (en) | 2011-11-22 |
| KR20030094357A (ko) | 2003-12-11 |
| JP2004536051A (ja) | 2004-12-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25G | Requested change of headquarter approved |
Owner name: DEBIOPHARM S.A. (CH) Free format text: SEDE ALTERADA CONFORME SOLICITADO NA PETICAO NO 057973/RJ DE 13/12/2004. |
|
| B25A | Requested transfer of rights approved |
Owner name: OPHTHALMOPHARMA AG (CH) Free format text: TRANSFERIDO DE: DEBIOPHARM S.A. |
|
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 13A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2308 DE 31/03/2015. |
|
| B07F | Notification of approval that there is no relation to art. 229 of lpi (pipeline patents) [chapter 7.6 patent gazette] |
Free format text: NOTIFICACAO DE NAO ANUENCIA RELACIONADA COM O ART. 229 DA LPI |