AR003922A1 - Compuestos de 1-[2-(metoxicarbonilamino)-3-metilburitil]-n-[2-metil-1- (trifluoroacetil)propil]pirrolidina-2-carboxamida, inhibidor de elastasa deneutrofila humana; composicion farmaceutica que lo contiene; proceso de fabricacion de dicho compuesto; compuesto de partida; proceso para la - Google Patents

Compuestos de 1-[2-(metoxicarbonilamino)-3-metilburitil]-n-[2-metil-1- (trifluoroacetil)propil]pirrolidina-2-carboxamida, inhibidor de elastasa deneutrofila humana; composicion farmaceutica que lo contiene; proceso de fabricacion de dicho compuesto; compuesto de partida; proceso para la

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Publication number
AR003922A1
AR003922A1 ARP960101257A AR10125796A AR003922A1 AR 003922 A1 AR003922 A1 AR 003922A1 AR P960101257 A ARP960101257 A AR P960101257A AR 10125796 A AR10125796 A AR 10125796A AR 003922 A1 AR003922 A1 AR 003922A1
Authority
AR
Argentina
Prior art keywords
pyrrolidine
methyl
compound
carboxamide
compounds
Prior art date
Application number
ARP960101257A
Other languages
English (en)
Original Assignee
Zeneca Ltd
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 Zeneca Ltd filed Critical Zeneca Ltd
Publication of AR003922A1 publication Critical patent/AR003922A1/es

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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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/10—Expectorants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

El presente invento se relaciona con formas particulares de una nueva 1-sustituido-N-[2-metil-1-(trifluoroacetil)propil]pirrolidina-2-carboxamida,las cuales son inhibidoras de la elastasa de leucocito humano (ELH), también conocida como elastasa neutrófila humana (ENH). En particular la invención serefiere a un compuesto de 1-[2-(metoxicarbonilamino)-3-metilbutiril]-N-[2-metil -1-(trifluoroacetil)propil]pirrolidina-2-carboxamida de la fórmula (I) o unaforma solvatada del mismo, o un cetal o hemicetal del mismo, como una mezcla diastereomérica que comprende 50% o más del diastereoisómero fórmula (Ia) o unaforma solvatada del mismo, o un cetal o hemicetal del mismo, en los cuales son útiles cuando se desee la inhibición de la ENH, tal como herramientas deinvestigación en estudios farmacológicos, de diagnóstico y relacionados y en el tratamiento de enfermedades en mamíferos en las cuales se ve implicada laENH. El invento también incluye composiciones farmacéuticas que contiene tales formas, procesos para preparar las formas y productos intermediosútiles en la síntesis de la formas y compuestos de partida.
ARP960101257A 1995-02-03 1996-02-02 Compuestos de 1-[2-(metoxicarbonilamino)-3-metilburitil]-n-[2-metil-1- (trifluoroacetil)propil]pirrolidina-2-carboxamida, inhibidor de elastasa deneutrofila humana; composicion farmaceutica que lo contiene; proceso de fabricacion de dicho compuesto; compuesto de partida; proceso para la AR003922A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9502152.3A GB9502152D0 (en) 1995-02-03 1995-02-03 Proline derivatives

Publications (1)

Publication Number Publication Date
AR003922A1 true AR003922A1 (es) 1998-09-30

Family

ID=10769064

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP960101257A AR003922A1 (es) 1995-02-03 1996-02-02 Compuestos de 1-[2-(metoxicarbonilamino)-3-metilburitil]-n-[2-metil-1- (trifluoroacetil)propil]pirrolidina-2-carboxamida, inhibidor de elastasa deneutrofila humana; composicion farmaceutica que lo contiene; proceso de fabricacion de dicho compuesto; compuesto de partida; proceso para la

Country Status (23)

Country Link
US (4) US5686628A (es)
EP (1) EP0808327A1 (es)
JP (1) JPH10513173A (es)
KR (1) KR19980701869A (es)
CN (1) CN1172486A (es)
AR (1) AR003922A1 (es)
AU (1) AU704704B2 (es)
BR (1) BR9607095A (es)
CA (1) CA2209675A1 (es)
CZ (1) CZ246697A3 (es)
FI (1) FI973211A (es)
GB (1) GB9502152D0 (es)
HR (1) HRP960008A2 (es)
HU (1) HUP9801991A3 (es)
IL (1) IL117013A0 (es)
NO (1) NO973539L (es)
NZ (1) NZ300256A (es)
PL (1) PL321680A1 (es)
RU (1) RU2159249C2 (es)
SK (1) SK105497A3 (es)
TR (1) TR199700732T1 (es)
WO (1) WO1996023812A1 (es)
ZA (1) ZA96851B (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6375926B1 (en) 1996-09-16 2002-04-23 Amersham International Plc Labelled elastase inhibitors
US5773430A (en) * 1997-03-13 1998-06-30 Research Foundation Of State University Of New York Serine proteinase inhibitory activity by hydrophobic tetracycline
US6559127B1 (en) 1997-07-31 2003-05-06 Athena Neurosciences, Inc. Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6489300B1 (en) 1997-07-31 2002-12-03 Eugene D. Thorsett Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4
US7030114B1 (en) 1997-07-31 2006-04-18 Elan Pharmaceuticals, Inc. Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6583139B1 (en) 1997-07-31 2003-06-24 Eugene D. Thorsett Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6362341B1 (en) 1997-07-31 2002-03-26 Athena Neurosciences, Inc. Benzyl compounds which inhibit leukocyte adhesion mediated by VLA-4
US6423688B1 (en) * 1997-07-31 2002-07-23 Athena Neurosciences, Inc. Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4
US6492421B1 (en) 1997-07-31 2002-12-10 Athena Neurosciences, Inc. Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
US7232918B2 (en) * 2001-11-06 2007-06-19 Shell Oil Company Catalyst composition
US6544732B1 (en) * 1999-05-20 2003-04-08 Illumina, Inc. Encoding and decoding of array sensors utilizing nanocrystals
ES2272258T3 (es) 1999-12-16 2007-05-01 Dainippon Sumitomo Pharma Co., Ltd. Procesos de produccion de derivados del (aminometil) trifluorometilcarbinol.
WO2006016720A1 (ja) * 2004-08-11 2006-02-16 Dainippon Sumitomo Pharma Co., Ltd. 医薬化合物
WO2006025216A1 (ja) * 2004-08-31 2006-03-09 Dainippon Sumitomo Pharma Co., Ltd. 医薬結晶化合物
GB2438319B (en) * 2005-02-08 2009-03-04 Smith International Thermally stable polycrystalline diamond cutting elements and bits incorporating the same
EP3517531B1 (en) * 2016-09-23 2021-02-24 Kaken Pharmaceutical Co., Ltd. Method for producing (r)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2h)-yl)methyl]imidazolidine-2,4-dione and intermediate for producing same
WO2021053058A1 (en) 2019-09-17 2021-03-25 Mereo Biopharma 4 Limited Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
MX2022012942A (es) 2020-04-16 2023-01-11 Mereo Biopharma 4 Ltd Metodos que involucran el inhibidor de la elastasa de neutrofilo alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina.
AU2022373971A1 (en) 2021-10-20 2024-04-04 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

Family Cites Families (9)

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Publication number Priority date Publication date Assignee Title
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
US5194588A (en) * 1985-01-22 1993-03-16 Ici Americas Inc. Aminoalcohol intermediates for peptide derivatives
US5055450A (en) * 1985-01-22 1991-10-08 Ici Americas Inc. Peptide derivatives
AU600226B2 (en) * 1985-02-04 1990-08-09 Merrell Pharmaceuticals Inc. Novel peptidase inhibitors
CH672792A5 (es) * 1985-02-19 1989-12-29 Sandoz Ag
GB9402680D0 (en) * 1994-02-11 1994-04-06 Zeneca Ltd Pyrrolidine derivatives

Also Published As

Publication number Publication date
NO973539D0 (no) 1997-08-01
GB9502152D0 (en) 1995-03-29
NO973539L (no) 1997-10-01
TR199700732T1 (xx) 1998-02-21
JPH10513173A (ja) 1998-12-15
EP0808327A1 (en) 1997-11-26
KR19980701869A (ko) 1998-06-25
HUP9801991A3 (en) 1999-06-28
AU704704B2 (en) 1999-04-29
NZ300256A (en) 2000-01-28
AU4494396A (en) 1996-08-21
CZ246697A3 (en) 1997-11-12
HUP9801991A2 (hu) 1999-02-01
WO1996023812A1 (en) 1996-08-08
FI973211A0 (fi) 1997-08-01
PL321680A1 (en) 1997-12-22
IL117013A0 (en) 1996-06-18
BR9607095A (pt) 1997-11-11
ZA96851B (en) 1996-08-05
US5808097A (en) 1998-09-15
CA2209675A1 (en) 1996-08-08
US6054593A (en) 2000-04-25
US6048889A (en) 2000-04-11
MX9705231A (es) 1997-10-31
CN1172486A (zh) 1998-02-04
US5686628A (en) 1997-11-11
RU2159249C2 (ru) 2000-11-20
SK105497A3 (en) 1997-12-10
HRP960008A2 (en) 1998-04-30
FI973211A (fi) 1997-08-01

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