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 laInfo
- 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
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
- C07K5/08—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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (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.
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) | FI973211A7 (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 (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6375926B1 (en) | 1996-09-16 | 2002-04-23 | Amersham International Plc | Labelled elastase inhibitors |
| HUP0100669A3 (en) * | 1996-12-06 | 2001-12-28 | Cortech Inc Denver | Peptide derivatives as serine protease inhibitors, their use and pharmaceutical compositions comprising thereof |
| US5773430A (en) * | 1997-03-13 | 1998-06-30 | Research Foundation Of State University Of New York | Serine proteinase inhibitory activity by hydrophobic tetracycline |
| US6362341B1 (en) | 1997-07-31 | 2002-03-26 | Athena Neurosciences, Inc. | Benzyl 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 |
| US6559127B1 (en) | 1997-07-31 | 2003-05-06 | Athena Neurosciences, Inc. | 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 |
| US7030114B1 (en) | 1997-07-31 | 2006-04-18 | Elan Pharmaceuticals, 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 |
| 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 |
| WO2001044165A1 (en) | 1999-12-16 | 2001-06-21 | Dainippon Pharmaceutical Co., Ltd. | Processes for producing (aminomethyl)trifluorocarbinol derivatives |
| US7294722B2 (en) * | 2002-12-12 | 2007-11-13 | Novartis Ag | Process for the synthesis of peptides containing a 4-hydroxy-proline substructure |
| 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 |
| US7533740B2 (en) * | 2005-02-08 | 2009-05-19 | Smith International Inc. | Thermally stable polycrystalline diamond cutting elements and bits incorporating the same |
| JP6934012B2 (ja) * | 2016-09-23 | 2021-09-08 | 科研製薬株式会社 | （ｒ）‐５‐（３，４‐ジフルオロフェニル）‐５‐［（３‐メチル‐２‐オキソピリジン‐１（２ｈ）‐イル）メチル］イミダゾリジン‐２，４‐ジオンの製造方法およびその製造のための中間体 |
| EP4031138A1 (en) | 2019-09-17 | 2022-07-27 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| AU2021256835A1 (en) | 2020-04-16 | 2022-10-13 | Mereo Biopharma 4 Limited | Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency |
| 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 (11)
| 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 |
| US4643991A (en) * | 1984-12-18 | 1987-02-17 | The University Of Kentucky Research Foundation | Peptide elastase inhibitors and methods |
| 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 |
| CA1341029C (en) * | 1985-02-04 | 2000-06-20 | Michael Kolb | Peptidase inhibitors |
| CH672792A5 (es) * | 1985-02-19 | 1989-12-29 | Sandoz Ag | |
| IT1203971B (it) * | 1987-04-24 | 1989-02-23 | Roussel Maestretti Spa | Derivati di 1,2,5,6-tetraidropiridina, loro procedimento di preparazione e loro applicazione come medicamenti |
| GB9402680D0 (en) * | 1994-02-11 | 1994-04-06 | Zeneca Ltd | Pyrrolidine derivatives |
-
1995
- 1995-02-03 GB GBGB9502152.3A patent/GB9502152D0/en active Pending
-
1996
- 1996-01-08 HR HR9502152.3A patent/HRP960008A2/hr not_active Application Discontinuation
- 1996-01-30 BR BR9607095A patent/BR9607095A/pt not_active Application Discontinuation
- 1996-01-30 JP JP8523340A patent/JPH10513173A/ja active Pending
- 1996-01-30 FI FI973211A patent/FI973211A7/fi unknown
- 1996-01-30 WO PCT/GB1996/000193 patent/WO1996023812A1/en not_active Ceased
- 1996-01-30 HU HU9801991A patent/HUP9801991A3/hu unknown
- 1996-01-30 CN CN96191721A patent/CN1172486A/zh active Pending
- 1996-01-30 RU RU97114890/04A patent/RU2159249C2/ru active
- 1996-01-30 CZ CZ972466A patent/CZ246697A3/cs unknown
- 1996-01-30 CA CA002209675A patent/CA2209675A1/en not_active Abandoned
- 1996-01-30 PL PL96321680A patent/PL321680A1/xx unknown
- 1996-01-30 KR KR1019970705266A patent/KR19980701869A/ko not_active Withdrawn
- 1996-01-30 NZ NZ300256A patent/NZ300256A/xx unknown
- 1996-01-30 TR TR97/00732T patent/TR199700732T1/xx unknown
- 1996-01-30 EP EP96901075A patent/EP0808327A1/en not_active Withdrawn
- 1996-01-30 SK SK1054-97A patent/SK105497A3/sk unknown
- 1996-01-30 AU AU44943/96A patent/AU704704B2/en not_active Ceased
- 1996-02-02 US US08/595,692 patent/US5686628A/en not_active Expired - Fee Related
- 1996-02-02 AR ARP960101257A patent/AR003922A1/es unknown
- 1996-02-02 IL IL11701396A patent/IL117013A0/xx unknown
- 1996-02-02 ZA ZA96851A patent/ZA96851B/xx unknown
-
1997
- 1997-08-01 NO NO973539A patent/NO973539L/no not_active Application Discontinuation
- 1997-08-22 US US08/918,626 patent/US5808097A/en not_active Expired - Fee Related
-
1998
- 1998-06-19 US US09/100,735 patent/US6054593A/en not_active Expired - Fee Related
-
1999
- 1999-03-23 US US09/274,572 patent/US6048889A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| ZA96851B (en) | 1996-08-05 |
| GB9502152D0 (en) | 1995-03-29 |
| AU704704B2 (en) | 1999-04-29 |
| NO973539D0 (no) | 1997-08-01 |
| NO973539L (no) | 1997-10-01 |
| SK105497A3 (en) | 1997-12-10 |
| FI973211L (fi) | 1997-08-01 |
| HUP9801991A3 (en) | 1999-06-28 |
| WO1996023812A1 (en) | 1996-08-08 |
| CA2209675A1 (en) | 1996-08-08 |
| NZ300256A (en) | 2000-01-28 |
| EP0808327A1 (en) | 1997-11-26 |
| FI973211A0 (fi) | 1997-08-01 |
| JPH10513173A (ja) | 1998-12-15 |
| CZ246697A3 (en) | 1997-11-12 |
| KR19980701869A (ko) | 1998-06-25 |
| FI973211A7 (fi) | 1997-08-01 |
| US5808097A (en) | 1998-09-15 |
| RU2159249C2 (ru) | 2000-11-20 |
| US6054593A (en) | 2000-04-25 |
| TR199700732T1 (xx) | 1998-02-21 |
| CN1172486A (zh) | 1998-02-04 |
| US6048889A (en) | 2000-04-11 |
| MX9705231A (es) | 1997-10-31 |
| PL321680A1 (en) | 1997-12-22 |
| US5686628A (en) | 1997-11-11 |
| BR9607095A (pt) | 1997-11-11 |
| AU4494396A (en) | 1996-08-21 |
| HUP9801991A2 (hu) | 1999-02-01 |
| IL117013A0 (en) | 1996-06-18 |
| HRP960008A2 (en) | 1998-04-30 |
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