CO4970719A1 - PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS - Google Patents
PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORSInfo
- Publication number
- CO4970719A1 CO4970719A1 CO98051488A CO98051488A CO4970719A1 CO 4970719 A1 CO4970719 A1 CO 4970719A1 CO 98051488 A CO98051488 A CO 98051488A CO 98051488 A CO98051488 A CO 98051488A CO 4970719 A1 CO4970719 A1 CO 4970719A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- carbon atoms
- optionally substituted
- halogen
- groups
- Prior art date
Links
- 239000003602 elastase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000004432 carbon atom Chemical group C* 0.000 abstract 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002785 azepinyl group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Un compuesto de la fórmula (I)(estereoquímica relativa indicada)en donde: R1 representa alquilo de 1 a 6 átomos de carbono; R2 representa alquilo de 2 a 4 átomos de carbono o alquenilo de 2 a 4 átomos de carbono; X representa CO o SO2 ; Het representa un sistema de anillo aromáticomonocíclico o bicíclico de 5 a 10 elementos, opcionalmente substituido, que contiene 1 a 4 heteroátomos seleccionados de O, N, y S; n representa un número entero de 0 a 4; R3 y R4 representan independientemente hidrógeno, alquilo de 1 a 8 átomos de carbono, -(CH2 )1-4 CONR5 R6 , COC1-4 alquilo o(CH2 )0-2 Fen en donde Fen representa fenilo opcionalmente sustituido por uno o más grupos alquilo de 1 a 4 átomos de carbono o grupos halógeno o NR3 R4 juntos representan azetidinilo, pirrolidinilo, piperidinilo, azepinilo, morfolinilo, piperazinilo opcionalmente N-susbtituido por alquilo de 1 a 6 átomos de carbono, fenilo(opcionalmente substituido por halógeno o alquilo de 1 a 4 átomos de carbono) o bencilo (opcionalmente substituido en el anillo de benceno por halógeno o alquilo de 1 a 4 átomos de carbono) o NR3 R4 juntos representan un anillo como se ha descrito hasta ahora salvo que se substituye en el carbono por uno o más grupos alquilo de 1 a 4 átomos de carbono, CONR5 R6 o COOR6 . R5 y R6 representan independientemente hidrógeno o alquilo de 1 a 4 átomos de carbono; y sales y solvatos de los mismos.A compound of formula (I) (indicated relative stereochemistry) wherein: R1 represents alkyl of 1 to 6 carbon atoms; R2 represents alkyl of 2 to 4 carbon atoms or alkenyl of 2 to 4 carbon atoms; X represents CO or SO2; Het represents an optionally substituted 5 to 10 membered bicyclic or bicyclic aromatic ring system containing 1 to 4 heteroatoms selected from O, N, and S; n represents an integer from 0 to 4; R3 and R4 independently represent hydrogen, alkyl of 1 to 8 carbon atoms, - (CH2) 1-4 CONR5 R6, COC1-4 alkyl or (CH2) 0-2 Fen where Fen represents phenyl optionally substituted by one or more groups C 1-4 -alkyl or halogen groups or NR3 R4 together represent azetidinyl, pyrrolidinyl, piperidinyl, azepinyl, morpholinyl, piperazinyl optionally N-substituted by C 1-6 -alkyl, phenyl (optionally substituted by halogen or alkyl of 1 to 4 carbon atoms) or benzyl (optionally substituted on the benzene ring by halogen or alkyl of 1 to 4 carbon atoms) or NR3 R4 together represent a ring as described so far except that it is substituted on carbon by one or more alkyl groups of 1 to 4 carbon atoms, CONR5 R6 or COOR6. R5 and R6 independently represent hydrogen or C1-C4-alkyl; and salts and solvates thereof.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9719189.4A GB9719189D0 (en) | 1997-09-09 | 1997-09-09 | New therapeutic method |
| GBGB9719183.7A GB9719183D0 (en) | 1997-09-09 | 1997-09-09 | Compounds |
| GBGB9719290.0A GB9719290D0 (en) | 1997-09-10 | 1997-09-10 | Compounds |
| GBGB9803611.4A GB9803611D0 (en) | 1998-02-21 | 1998-02-21 | Compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO4970719A1 true CO4970719A1 (en) | 2000-11-07 |
Family
ID=27451698
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO98051488A CO4970719A1 (en) | 1997-09-09 | 1998-09-08 | PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP1003748A2 (en) |
| JP (1) | JP2001515904A (en) |
| KR (1) | KR20010023766A (en) |
| CN (1) | CN1278820A (en) |
| AP (1) | AP2000001761A0 (en) |
| AR (1) | AR017072A1 (en) |
| AU (1) | AU9741298A (en) |
| BR (1) | BR9812062A (en) |
| CA (1) | CA2303176A1 (en) |
| CO (1) | CO4970719A1 (en) |
| EA (1) | EA200000204A1 (en) |
| EE (1) | EE200000138A (en) |
| HU (1) | HUP0004644A3 (en) |
| ID (1) | ID24452A (en) |
| IL (1) | IL134791A0 (en) |
| IS (1) | IS5391A (en) |
| MA (1) | MA26543A1 (en) |
| NO (1) | NO20001198L (en) |
| NZ (1) | NZ503130A (en) |
| PE (1) | PE107899A1 (en) |
| PL (1) | PL339176A1 (en) |
| SK (1) | SK3192000A3 (en) |
| TR (1) | TR200000907T2 (en) |
| WO (1) | WO1999012933A2 (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9905418D0 (en) * | 1999-03-09 | 1999-05-05 | Glaxo Group Ltd | Process |
| AU2005231375A1 (en) | 2004-03-31 | 2005-10-20 | Janssen Pharmaceutica, N.V. | Non-imidazole heterocyclic compounds as histamine H3 receptor modulators |
| DE102004024772A1 (en) * | 2004-05-17 | 2005-12-22 | Grünenthal GmbH | Substituted 5-aminomethyl-1H-pyrrole-2-carboxamides |
| JP4853759B2 (en) * | 2004-05-27 | 2012-01-11 | 日本農薬株式会社 | Substituted pyrazinecarboxylic acid anilide derivatives or salts thereof, intermediates thereof, agricultural and horticultural agents, and methods of use thereof |
| TWI355380B (en) * | 2004-05-27 | 2012-01-01 | Nihon Nohyaku Co Ltd | Substituted pyrazinecarboxanilide derivatives or s |
| GB2418427A (en) | 2004-09-02 | 2006-03-29 | Univ Cambridge Tech | Ligands for G-protein coupled receptors |
| ES2328384T3 (en) | 2004-11-23 | 2009-11-12 | Warner-Lambert Company Llc | ACID DERIVATIVES 7- (2H-PIRAZOL-3-IL) -3,5-DIHIDROXI-HEPTANOICO AS INHIBITORS OF HMG CO-A REDUCTASE FOR THE TREATMENT OF LIPIDEMIA. |
| DE602007009095D1 (en) | 2006-05-04 | 2010-10-21 | Pulmagen Therapeutics Inflamma | TETRAHYDROPYRROLOPYRIMIDINDIONE AND ITS USE AS INHIBITORS OF HUMAN NEUTROPHIL ELASTASE |
| US8198288B2 (en) | 2006-05-04 | 2012-06-12 | Pulmagen Therapeutics (Inflammation) Limited | Tetrahydropyrrolopyrimidinediones and their use in therapy |
| US7662967B2 (en) | 2007-08-02 | 2010-02-16 | Cambridge Enterprise Limited | Anti-inflammatory compounds and compositions |
| GB2452696B (en) | 2007-08-02 | 2009-09-23 | Cambridge Entpr Ltd | 3-(2',2'-dimethylpropanoylamino)-tetrahydropyridin-2-one and its use in pharmaceutical compositions |
| WO2009060206A1 (en) * | 2007-11-07 | 2009-05-14 | Argenta Discovery Limited | 3,4,6,7-tetrahydro-1h-pyrrolo[3,4-d]pyrimidine-2,5-diones and their therapeutic use |
| US20110212181A1 (en) * | 2010-02-26 | 2011-09-01 | The University Of Hong Kong | Compositions and methods for treating chronic respiratory inflammation |
| 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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9211783D0 (en) * | 1992-06-04 | 1992-07-15 | Ici Plc | Amide derivatives |
| GB9402680D0 (en) * | 1994-02-11 | 1994-04-06 | Zeneca Ltd | Pyrrolidine derivatives |
| AR006401A1 (en) * | 1996-03-28 | 1999-08-25 | Glaxo Group Ltd | PIRROLOPYROLONE COMPOUNDS, A PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM, ITS USE IN THE MANUFACTURE OF A MEDICINAL PRODUCT AND IN THERAPY, PROCESSES FOR ITS PREPARATION AND INTERMEDIARY COMPOUNDS FOR SUCH PROCESSES. |
-
1998
- 1998-09-04 PE PE1998000828A patent/PE107899A1/en not_active Application Discontinuation
- 1998-09-07 PL PL98339176A patent/PL339176A1/en not_active Application Discontinuation
- 1998-09-07 IL IL13479198A patent/IL134791A0/en unknown
- 1998-09-07 EE EEP200000138A patent/EE200000138A/en unknown
- 1998-09-07 WO PCT/EP1998/005609 patent/WO1999012933A2/en not_active Ceased
- 1998-09-07 ID IDW20000445A patent/ID24452A/en unknown
- 1998-09-07 JP JP2000510740A patent/JP2001515904A/en active Pending
- 1998-09-07 CN CN98810954A patent/CN1278820A/en active Pending
- 1998-09-07 MA MA25243A patent/MA26543A1/en unknown
- 1998-09-07 KR KR1020007002422A patent/KR20010023766A/en not_active Withdrawn
- 1998-09-07 EP EP98951348A patent/EP1003748A2/en not_active Withdrawn
- 1998-09-07 AP APAP/P/2000/001761A patent/AP2000001761A0/en unknown
- 1998-09-07 CA CA002303176A patent/CA2303176A1/en not_active Abandoned
- 1998-09-07 TR TR2000/00907T patent/TR200000907T2/en unknown
- 1998-09-07 HU HU0004644A patent/HUP0004644A3/en unknown
- 1998-09-07 BR BR9812062-0A patent/BR9812062A/en not_active Application Discontinuation
- 1998-09-07 NZ NZ503130A patent/NZ503130A/en unknown
- 1998-09-07 EA EA200000204A patent/EA200000204A1/en unknown
- 1998-09-07 AU AU97412/98A patent/AU9741298A/en not_active Abandoned
- 1998-09-07 AR ARP980104458A patent/AR017072A1/en unknown
- 1998-09-07 SK SK319-2000A patent/SK3192000A3/en unknown
- 1998-09-08 CO CO98051488A patent/CO4970719A1/en unknown
-
2000
- 2000-02-29 IS IS5391A patent/IS5391A/en unknown
- 2000-03-08 NO NO20001198A patent/NO20001198L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| IL134791A0 (en) | 2001-04-30 |
| PL339176A1 (en) | 2000-12-04 |
| CN1278820A (en) | 2001-01-03 |
| NZ503130A (en) | 2001-08-31 |
| SK3192000A3 (en) | 2001-03-12 |
| WO1999012933A3 (en) | 1999-05-27 |
| PE107899A1 (en) | 1999-11-17 |
| AR017072A1 (en) | 2001-08-22 |
| BR9812062A (en) | 2000-09-26 |
| NO20001198D0 (en) | 2000-03-08 |
| KR20010023766A (en) | 2001-03-26 |
| TR200000907T2 (en) | 2000-11-21 |
| EE200000138A (en) | 2001-02-15 |
| AU9741298A (en) | 1999-03-29 |
| EA200000204A1 (en) | 2000-10-30 |
| IS5391A (en) | 2000-02-29 |
| NO20001198L (en) | 2000-05-08 |
| CA2303176A1 (en) | 1999-03-18 |
| WO1999012933A2 (en) | 1999-03-18 |
| HUP0004644A3 (en) | 2002-01-28 |
| AP2000001761A0 (en) | 2000-03-31 |
| ID24452A (en) | 2000-07-20 |
| MA26543A1 (en) | 2004-12-20 |
| EP1003748A2 (en) | 2000-05-31 |
| JP2001515904A (en) | 2001-09-25 |
| HUP0004644A2 (en) | 2001-09-28 |
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