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 a2

Info

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
Application number
ES09200809A
Other languages
English (en)
Other versions
ES2044781A1 (es
Inventor
Germano Carganico
Casellas David Mauleon
Perez M Luisa Garcia
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Laboratorios Menarini SA
Original Assignee
Laboratorios Menarini SA
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Laboratorios Menarini SA filed Critical Laboratorios Menarini SA
Priority to ES09200809A priority Critical patent/ES2044781B1/es
Priority to AU39525/93A priority patent/AU3952593A/en
Priority to PCT/EP1993/000866 priority patent/WO1993021211A1/en
Publication of ES2044781A1 publication Critical patent/ES2044781A1/es
Application granted granted Critical
Publication of ES2044781B1 publication Critical patent/ES2044781B1/es
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

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.
ES09200809A 1992-04-14 1992-04-14 Procedimiento para la preparacion de nuevas amidas con accion inhibidora de la fosfolipasa a2 Expired - Fee Related ES2044781B1 (es)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU708306B2 (en) * 1995-07-24 1999-07-29 Fujisawa Pharmaceutical Co., Ltd. Esters and amides as PLA2 inhibitors
KR19990035780A (ko) * 1995-07-24 1999-05-25 후지야마 아키라 Ｐｌａ２ 억제제로서의 에스테르 및 아미드
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
WO2006054304A2 (en) * 2004-11-17 2006-05-26 Yissum Research Development Company Of The Hebrew University Of Jerusalem Use of lipid conjugates in the treatment of disease
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
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
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
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
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
WO2002076485A2 (en) 2001-03-27 2002-10-03 Biomira, Inc. Vaccine for modulating between t1 and t2 immune responses
WO2003089574A2 (en) * 2002-04-15 2003-10-30 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
PT1896051E (pt) 2005-06-28 2015-01-13 Oncothyreon Inc Método de tratamento de pacientes com uma vacina de glicoproteína mucinosa (muc-1)
CN105193724A (zh) 2011-02-24 2015-12-30 肿瘤防护公司 含有佐剂的以muc1 为基础的糖脂肽疫苗
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
ES2044781A1 (es) 1994-01-01
AU3952593A (en) 1993-11-18
WO1993021211A1 (en) 1993-10-28

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Legal Events

Date Code Title Description
FD1A Patent lapsed

Effective date: 20060415