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ES8802619A1 - Procedimiento para preparar peptidos difluorcetonicos - Google Patents

Procedimiento para preparar peptidos difluorcetonicos

Info

Publication number
ES8802619A1
ES8802619A1 ES557733A ES557733A ES8802619A1 ES 8802619 A1 ES8802619 A1 ES 8802619A1 ES 557733 A ES557733 A ES 557733A ES 557733 A ES557733 A ES 557733A ES 8802619 A1 ES8802619 A1 ES 8802619A1
Authority
ES
Spain
Prior art keywords
alkyl
ceto
amino
difluoro derivatives
hydroxibenzotria
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
Application number
ES557733A
Other languages
English (en)
Other versions
ES557733A0 (es
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.)
Zeneca Inc
Original Assignee
ICI Americas Inc
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
Priority claimed from GB858514438A external-priority patent/GB8514438D0/en
Priority claimed from GB858514440A external-priority patent/GB8514440D0/en
Priority claimed from GB858514436A external-priority patent/GB8514436D0/en
Application filed by ICI Americas Inc filed Critical ICI Americas Inc
Publication of ES8802619A1 publication Critical patent/ES8802619A1/es
Publication of ES557733A0 publication Critical patent/ES557733A0/es
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/18Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Detergent Compositions (AREA)
  • Cosmetics (AREA)

Abstract

LOS PEPTIDOS DIFLUORCETONICOS (I), (II) Y (III), DONDE NO EXCLUSIVAMENTE, R1 ES ALQUILO C1-5, R2 ALQUILO C1-6 SUSTITUIDO POR AMINO, HIDROXI O ARILO CONTENIENDO C6, C10 O C12, R3 ALQUILO C1-12, Y OPCIONALMENTE DE 1 A 4 HETEROATOMOS, A ES CETO, AMIDO, ESTER, RA ES RB.NRC.CO CON R3 ALQUILO C1-10, RC HIDROGENO O METILO; SE OBTIENEN HACIENDO REACCIONAR UN AMINO CETO ACIDO DIFLUORADO (IV) DONDE Q ES UN GRUPO (V), CON UNA AMINA RB.NH.RC POR ACOPLAMIENTO CON CARBODIIMIDA SOLUBLE EN AGUA NORMALIZADA U 1-HIDROXIBENZOTRIAZOL EN UN DISLUYENTE ADECUADO COMO TETRAHIDROFURANO ENTRE 0 Y 35GC. SON INHIBIDORES DE LA ELASTASA DE LEUCOCITOS HUMANOS (HLE) APLICABLES AL TRATAMIENTO DEL ENFISEMA PULMONAR, ATEROSCLEROSIS, ARTRITIS REUMATOIDE Y OSTEOARTRITIS. *FORMULA* N
ES557733A 1985-06-07 1987-09-16 Procedimiento para preparar peptidos difluorcetonicos Expired ES8802619A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB858514438A GB8514438D0 (en) 1985-06-07 1985-06-07 Selected difluoro ketone dipeptide derivatives
GB858514440A GB8514440D0 (en) 1985-06-07 1985-06-07 Difluoro ketone tripeptide derivatives
GB858514436A GB8514436D0 (en) 1985-06-07 1985-06-07 Selected difluoro derivatives

Publications (2)

Publication Number Publication Date
ES8802619A1 true ES8802619A1 (es) 1988-09-01
ES557733A0 ES557733A0 (es) 1988-09-01

Family

ID=27262698

Family Applications (4)

Application Number Title Priority Date Filing Date
ES555826A Expired ES8801305A1 (es) 1985-06-07 1986-06-06 Procedimiento para preparar peptidos difluorcetonicos
ES557734A Expired ES8900051A1 (es) 1985-06-07 1987-09-16 Procedimiento para preparar peptidos difluorcetonicos
ES557733A Expired ES8802619A1 (es) 1985-06-07 1987-09-16 Procedimiento para preparar peptidos difluorcetonicos
ES557735A Expired ES8802321A1 (es) 1985-06-07 1987-09-16 Procedimiento para preparar peptidos difluorcetonicos

Family Applications Before (2)

Application Number Title Priority Date Filing Date
ES555826A Expired ES8801305A1 (es) 1985-06-07 1986-06-06 Procedimiento para preparar peptidos difluorcetonicos
ES557734A Expired ES8900051A1 (es) 1985-06-07 1987-09-16 Procedimiento para preparar peptidos difluorcetonicos

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES557735A Expired ES8802321A1 (es) 1985-06-07 1987-09-16 Procedimiento para preparar peptidos difluorcetonicos

Country Status (16)

Country Link
US (1) US4880780A (es)
EP (1) EP0204571B1 (es)
JP (1) JPH07116159B2 (es)
AT (1) ATE71934T1 (es)
AU (1) AU594683B2 (es)
DE (1) DE3683541D1 (es)
DK (1) DK267686A (es)
ES (4) ES8801305A1 (es)
FI (1) FI86859C (es)
GR (1) GR861488B (es)
HU (1) HU208438B (es)
IE (1) IE59146B1 (es)
IL (1) IL79049A0 (es)
NO (1) NO170585C (es)
NZ (1) NZ216437A (es)
PT (1) PT82724B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8600263D0 (en) * 1985-01-22 1986-02-12 Ici America Inc Peptide derivatives
US5496927A (en) * 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
GB8711748D0 (en) * 1986-06-05 1987-06-24 Ici America Inc Difluoro keto compounds
GB8613703D0 (en) * 1986-06-05 1986-07-09 Ici America Inc Difluoro peptide compounds
GB8809316D0 (en) * 1987-05-11 1988-05-25 Ici America Inc Heterocyclic ketones
EP0371179A1 (en) * 1988-10-28 1990-06-06 Merrell Dow Pharmaceuticals Inc. Novel analogs of peptidase substrates
EP0369391A3 (en) * 1988-11-15 1991-09-25 Boehringer Ingelheim Pharmaceuticals Inc. N-substituted amides
GB8910547D0 (en) * 1989-05-08 1989-06-21 Ici America Inc Substituted ketones
US5221665A (en) * 1989-10-27 1993-06-22 Boehringer Ingelheim Pharmaceuticals, Inc. N-substituted amides
US5391705A (en) * 1991-03-15 1995-02-21 Merrell Dow Pharmaceuticals Inc. Polyfluorinated tripeptide thrombin inhibitors
AU655301B2 (en) * 1991-05-23 1994-12-15 Merrell Pharmaceuticals Inc. Inhibitors of cathepsin G and elastase for preventing connective tissue degradation
US5478811A (en) * 1991-08-22 1995-12-26 Merrell Dow Pharmaceuticals Inc. Orally-active elastase inhibitors
US5714470A (en) 1991-08-22 1998-02-03 Merrell Pharmaceuticals, Inc. Orally-active elastase inhibitors
US5486529A (en) * 1992-04-16 1996-01-23 Zeneca Limited Certain pyridyl ketones for treating diseases involving leukocyte elastase
IL108031A0 (en) * 1992-12-22 1994-04-12 Procter & Gamble Difluoro pentapeptide derivatives and pharmaceutical compositions containing them
US6008196A (en) * 1994-06-02 1999-12-28 Hoechst Marion Roussel, Inc. Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
JP4221059B2 (ja) * 1994-06-02 2009-02-12 アベンティス・インコーポレイテッド エラスターゼインヒビターのプロドラッグとしてのアシル化エノール誘導体
PT804465E (pt) * 1994-06-02 2003-12-31 Aventis Pharma Inc Novos inibidores da elastase
US6069232A (en) * 1995-10-02 2000-05-30 Hoechst Marion Roussel, Inc. Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors
US5948886A (en) * 1996-11-20 1999-09-07 Hoechst Marion Roussel, Inc. Acylated enol derivatives of α-ketoesters and α-ketoamides
US6172044B1 (en) 1995-12-01 2001-01-09 Aventis Pharmaceuticals Inc. Acylated enol derivative of α-ketoesters and α-ketoamides
US6673784B1 (en) 1996-03-19 2004-01-06 G. D. Searle & Co. Electrophilic ketones for the treatment of herpesvirus infections
US5739354A (en) * 1996-03-26 1998-04-14 Hoechst Marion Roussel, Inc. Process for the preparation of N-methyl-D-phenylalanyl-N- 1- 3- (aminoiminomethyl)amino!propyl!-3,3-difluoro-2-oxohexyl!-L-prolinamide
EP0932617B1 (en) 1996-10-18 2002-01-16 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
AR055395A1 (es) 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
NZ571280A (en) * 2006-03-16 2011-10-28 Vertex Pharma Deuterated hepatitis C protease inhibitors
US8754107B2 (en) * 2006-11-17 2014-06-17 Abbvie Inc. Aminopyrrolidines as chemokine receptor antagonists
AU2008219704A1 (en) 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
AR065498A1 (es) 2007-02-27 2009-06-10 Vertex Pharma Co- critales de vx-950 (un inhibidor del virus de la hepatitis c) y composiciones farmaceuticas que los comprenden
AU2008297015B2 (en) 2007-08-30 2013-08-22 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
MY159837A (en) 2009-08-29 2017-02-15 Abbvie Inc Therapeutic dll4 binding proteins
SG183872A1 (en) 2010-03-02 2012-11-29 Abbvie Inc Therapeutic dll4 binding proteins
BR112013002578A2 (pt) 2010-08-03 2019-05-14 Abbvie Inc. imunoglobinas de domínio variável duplo e usos das mesmas
TW202210507A (zh) 2012-11-01 2022-03-16 美商艾伯維有限公司 抗-vegf/dll4雙重可變區域免疫球蛋白及其用途
WO2016094881A2 (en) 2014-12-11 2016-06-16 Abbvie Inc. Lrp-8 binding proteins
CN107531653B (zh) * 2015-05-11 2021-10-19 豪夫迈·罗氏有限公司 新的二氟酮酰胺衍生物
TW201710286A (zh) 2015-06-15 2017-03-16 艾伯維有限公司 抗vegf、pdgf及/或其受體之結合蛋白
MX2021015894A (es) * 2019-07-01 2022-02-03 Basf Se Peptidos acetales para estabilizar enzimas.

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE787249A (fr) 1971-08-05 1973-02-05 Squibb & Sons Inc Derives amino d'acides pyrazolopyridine carboxyliques, leurs esters et les sels de ces composes, ainsi que leurs procedes de preparation
US3935280A (en) 1975-01-10 1976-01-27 Aldrich-Boranes, Inc. Reduction of amino acids in the presence of boron trifluoride
US4277395A (en) * 1980-06-16 1981-07-07 Richardson-Merrell Inc. Novel enzyme inhibitors
DE3481913D1 (de) 1983-04-27 1990-05-17 Ici America Inc Prolin-derivate.
US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
GB8600263D0 (en) * 1985-01-22 1986-02-12 Ici America Inc Peptide derivatives

Also Published As

Publication number Publication date
FI862434A0 (fi) 1986-06-06
FI862434A7 (fi) 1986-12-08
ES555826A0 (es) 1987-12-16
IE59146B1 (en) 1994-01-12
ES8802321A1 (es) 1988-05-01
JPH07116159B2 (ja) 1995-12-13
FI86859C (fi) 1992-10-26
PT82724B (pt) 1988-12-15
AU5845486A (en) 1986-12-18
ES8801305A1 (es) 1987-12-16
DK267686D0 (da) 1986-06-06
PT82724A (en) 1986-07-01
NO862269L (no) 1986-12-08
EP0204571B1 (en) 1992-01-22
ES557734A0 (es) 1988-11-16
ES8900051A1 (es) 1988-11-16
ATE71934T1 (de) 1992-02-15
GR861488B (en) 1986-09-05
EP0204571A3 (en) 1988-09-21
HUT40811A (en) 1987-02-27
ES557733A0 (es) 1988-09-01
IL79049A0 (en) 1986-09-30
EP0204571A2 (en) 1986-12-10
ES557735A0 (es) 1988-05-01
FI86859B (fi) 1992-07-15
HU208438B (en) 1993-10-28
DE3683541D1 (de) 1992-03-05
AU594683B2 (en) 1990-03-15
JPS6253951A (ja) 1987-03-09
NO862269D0 (no) 1986-06-06
NZ216437A (en) 1990-06-26
NO170585B (no) 1992-07-27
IE861513L (en) 1986-12-07
DK267686A (da) 1986-12-08
US4880780A (en) 1989-11-14
NO170585C (no) 1992-11-04

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