ES2044781B1 - Procedimiento para la preparacion de nuevas amidas con accion inhibidora de la fosfolipasa a2 - Google Patents
Procedimiento para la preparacion de nuevas amidas con accion inhibidora de la fosfolipasa a2Info
- Publication number
- ES2044781B1 ES2044781B1 ES09200809A ES9200809A ES2044781B1 ES 2044781 B1 ES2044781 B1 ES 2044781B1 ES 09200809 A ES09200809 A ES 09200809A ES 9200809 A ES9200809 A ES 9200809A ES 2044781 B1 ES2044781 B1 ES 2044781B1
- Authority
- ES
- Spain
- Prior art keywords
- phospholipase
- procedure
- preparation
- alkyl
- hydrogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 150000001408 amides Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- 102100037611 Lysophospholipase Human genes 0.000 title 1
- 108010058864 Phospholipases A2 Proteins 0.000 title 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- ZIIUUSVHCHPIQD-UHFFFAOYSA-N 2,4,6-trimethyl-N-[3-(trifluoromethyl)phenyl]benzenesulfonamide Chemical compound CC1=CC(C)=CC(C)=C1S(=O)(=O)NC1=CC=CC(C(F)(F)F)=C1 ZIIUUSVHCHPIQD-UHFFFAOYSA-N 0.000 abstract 2
- 102000015439 Phospholipases Human genes 0.000 abstract 2
- 108010064785 Phospholipases Proteins 0.000 abstract 2
- 101100217226 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) ASI2 gene Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- KKFDJZZADQONDE-UHFFFAOYSA-N (hydridonitrato)hydroxidocarbon(.) Chemical class O[C]=N KKFDJZZADQONDE-UHFFFAOYSA-N 0.000 abstract 1
- 206010002199 Anaphylactic shock Diseases 0.000 abstract 1
- 101100316752 Arabidopsis thaliana VAL1 gene Proteins 0.000 abstract 1
- -1 CARBOXYL Chemical class 0.000 abstract 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical class [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 1
- 101100467813 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) RBS1 gene Proteins 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical class O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 1
- 230000003213 activating effect Effects 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 208000003455 anaphylaxis Diseases 0.000 abstract 1
- 230000003266 anti-allergic effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000002785 anti-thrombosis Effects 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000001681 protective effect Effects 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
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
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
- C07K5/06069—Ser-amino acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
PROCEDIMIENTO PARA LA PREPARACION DE NUEVAS AMIDAS CON ACCION INHIBIDORA DE LA FOSFOLIPASA ASI2 SC. LA PRESENTE INVENCION SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION DE NUEVAS AMIDAS DE FORMULA GENERAL I, FORMULA DONDE X ES OXIGENO O AZUFRE RBS1 SC ES ALQUILO; RBS2 SC ES HIDROGENO, ALQUILCARBONILO, ALCOXICARBONILO O ALQUILSULFONILO; RBS3 SC ES HIDROGENO, CARBOXILO, ALCOXICARBONILO O ARILOXICARBONILO; Y RBS4 SC HIDROGENO, ALQUILO, ARILALQUILO, HIDROXIALQUILO, TIOALQUILO, AMINOALQUILO, CARBOXIALQUILO, CARBAMOILO, GUANIDINOALQUILO O SULFOALQUILO. DICHAS AMIDAS SE OBTIENEN HACIENDO REACCIONAR UN COMPUESTO II, DONDE RBS6 SC EQUIVALE A RBS2 SC O ES UN GRUPO PROTECTOR ADECUADO, CON UNA AMINA APROPIADA HSI2 SCNCHRBS3 SCRBS4 SC, EN PRESENCIA DE UNA BASE CAPTADORA DE PROTONES Y UN AGENTE ACTIVANTE DE GRUPOS CARBOXILOS. DICHOS COMPUESTOS SON INHIBIDORES DE LA FOSFOLIPASA ASI2 SC, PUDIENDO SER UTILIZADOSCOMO ANTIINFLAMATORIOS, ANTIALERGICOS, ANTITROMBOTICOS, ANTIASMATICOS Y EN LA PREVENCION DELSHOCK ANAFILACTICO.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES09200809A ES2044781B1 (es) | 1992-04-14 | 1992-04-14 | Procedimiento para la preparacion de nuevas amidas con accion inhibidora de la fosfolipasa a2 |
| AU39525/93A AU3952593A (en) | 1992-04-14 | 1993-04-07 | Amides having inhibiting activity on phospholipase A2, a process for the preparation thereof and pharmaceutical compositions containing them |
| PCT/EP1993/000866 WO1993021211A1 (en) | 1992-04-14 | 1993-04-07 | Amides having inhibiting activity on phospholipase a2, a process for the preparation thereof and pharmaceutical compositions containing them |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES09200809A ES2044781B1 (es) | 1992-04-14 | 1992-04-14 | Procedimiento para la preparacion de nuevas amidas con accion inhibidora de la fosfolipasa a2 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2044781A1 ES2044781A1 (es) | 1994-01-01 |
| ES2044781B1 true ES2044781B1 (es) | 1994-10-01 |
Family
ID=8276745
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09200809A Expired - Fee Related ES2044781B1 (es) | 1992-04-14 | 1992-04-14 | Procedimiento para la preparacion de nuevas amidas con accion inhibidora de la fosfolipasa a2 |
Country Status (3)
| Country | Link |
|---|---|
| AU (1) | AU3952593A (es) |
| ES (1) | ES2044781B1 (es) |
| WO (1) | WO1993021211A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020019416A1 (en) | 1995-07-24 | 2002-02-14 | Naoki Fukami | Esters and amides as pla2 inhibitors |
| AU708306B2 (en) * | 1995-07-24 | 1999-07-29 | Fujisawa Pharmaceutical Co., Ltd. | Esters and amides as PLA2 inhibitors |
| US8916539B2 (en) | 2000-01-10 | 2014-12-23 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of lipid conjugates in the treatment of disease |
| US7893226B2 (en) | 2004-09-29 | 2011-02-22 | Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. | Use of lipid conjugates in the treatment of diseases |
| US7772196B2 (en) | 2000-01-10 | 2010-08-10 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of lipid conjugates in the treatment of diseases |
| US9040078B2 (en) | 2000-01-10 | 2015-05-26 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of lipid conjugates in the treatment of diseases of the nervous system |
| US7608598B2 (en) | 2000-01-10 | 2009-10-27 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of lipid conjugates in the treatment of conjunctivitis |
| US8883761B2 (en) | 2001-01-10 | 2014-11-11 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of lipid conjugates in the treatment of diseases associated with vasculature |
| US8198400B2 (en) | 2001-03-27 | 2012-06-12 | Oncothyreon, Inc. | Vaccine for modulating between T1 and T2 immune responses |
| US20060069238A1 (en) * | 2002-04-15 | 2006-03-30 | Biomira, Inc. | Synthetic glyco-lipo-peptides as vaccines |
| TWI395591B (zh) | 2004-04-01 | 2013-05-11 | Oncothyreon Inc | 黏液性糖蛋白(muc-1)疫苗 |
| EA012138B1 (ru) * | 2004-11-17 | 2009-08-28 | Йиссум Рисерч Дивелопмент Компани Оф Дзе Хебрю Юниверсити Оф Иерусалим | Применение конъюгатов липидов при лечении заболеваний |
| ES2526344T3 (es) | 2005-06-28 | 2015-01-09 | Oncothyreon Inc. | Método para el tratamiento de pacientes con una vacuna de glicoproteína mucinosa (MUC-1) |
| KR20140023903A (ko) | 2011-02-24 | 2014-02-27 | 온코타이레온, 인코포레이티드 | 항원보강제를 갖는 muc1 기초 당지질펩티드 백신 |
| CN105152986B (zh) * | 2015-09-09 | 2017-08-25 | 武汉华纳联合药业有限公司 | 半胱氨酸‑高牛磺酸二肽及其衍生物及其医药用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1964798A1 (de) * | 1969-01-07 | 1970-07-16 | Ciba Geigy | Neue pharmazeutische Praeparate |
| NL175293C (nl) * | 1972-02-08 | 1984-10-16 | Akzo Nv | Werkwijze ter bereiding of vervaardiging van een farmaceutisch preparaat met psychofarmacologische werking, alsmede werkwijze voor het bereiden van een van vasopressine afgeleid peptide. |
| US4111924A (en) * | 1976-01-05 | 1978-09-05 | Takeda Chemical Industries, Ltd. | Method for removal of thiol-protecting groups |
| IL84252A (en) * | 1987-10-23 | 1994-02-27 | Yissum Res Dev Co | Phospholipase inhibiting compositions |
-
1992
- 1992-04-14 ES ES09200809A patent/ES2044781B1/es not_active Expired - Fee Related
-
1993
- 1993-04-07 AU AU39525/93A patent/AU3952593A/en not_active Abandoned
- 1993-04-07 WO PCT/EP1993/000866 patent/WO1993021211A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| AU3952593A (en) | 1993-11-18 |
| WO1993021211A1 (en) | 1993-10-28 |
| ES2044781A1 (es) | 1994-01-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD1A | Patent lapsed |
Effective date: 20060415 |