PE20000725A1 - ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS - Google Patents
ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORSInfo
- Publication number
- PE20000725A1 PE20000725A1 PE1999000518A PE00051899A PE20000725A1 PE 20000725 A1 PE20000725 A1 PE 20000725A1 PE 1999000518 A PE1999000518 A PE 1999000518A PE 00051899 A PE00051899 A PE 00051899A PE 20000725 A1 PE20000725 A1 PE 20000725A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compounds
- het
- alcoxypyrrolidinone
- preferred
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- ZYVYEJXMYBUCMN-UHFFFAOYSA-N 1-methoxy-2-methylpropane Chemical class COCC(C)C ZYVYEJXMYBUCMN-UHFFFAOYSA-N 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- PUJDIJCNWFYVJX-UHFFFAOYSA-N benzyl carbamate Chemical compound NC(=O)OCC1=CC=CC=C1 PUJDIJCNWFYVJX-UHFFFAOYSA-N 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 210000000845 cartilage Anatomy 0.000 abstract 1
- 230000015556 catabolic process Effects 0.000 abstract 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 abstract 1
- 238000006731 degradation reaction Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000024693 gingival disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000028169 periodontal disease Diseases 0.000 abstract 1
- 201000001245 periodontitis Diseases 0.000 abstract 1
- 229940121649 protein inhibitor Drugs 0.000 abstract 1
- 239000012268 protein inhibitor Substances 0.000 abstract 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic 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
- C07D207/18—Heterocyclic 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 one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic 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 one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (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)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cosmetics (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS ALCOXIPIRROLIDINONA DE FORMULA I, DONDE X ES O, S, SO, SO2; Y ES H2, O; R1 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, (CH2)(0-6)CO2R", DE PREFERENCIA GRUPO a, b; R" ES H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, HET-ALQUILO C0-C6, DE PREFERENCIA ISOBUTILO, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, DE PREFERENCIA GRUPO c, d; Ar ES FENILO, NAFTILO, OPCIONALMENTE SUSTITUIDO CON Ph-ALQUILO C0-C6, HET-ALQUILO C0-C6, O(CH2)(1-6)NR`R', ENTRE OTROS; R' ES H, ALQUILO C1-C6, ENTRE OTROS; HET ES UN ANILLO HETEROCICLICO BICICLICO DE 7-10 MIEMBROS, ANILLO MONICICLICO DE 5-7 MIEMBROS OPCIONALMENTE SUSTITUIDO CON OR', N(R')2, SR'CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 3-BENCILOXI-1-(N-CARBOBENCILOXI-L-LEUCINIL)PIRROLIDIN-4-ONA, 1-[2-(BENCILOXICARBONILAMINO)-4-METILPENTIL]-3-BENCILTIO-4-HIDROXIPIRROLIDINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA CONVERTIR 3-BENCILOXI-4-HIDROXI-1-(N-CARBOBENCILOXI-L-LEUCINIL)PIRROLIDONA, ENTRE OTROS EN UN COMPUESTO DE FORMULA I. EL COMPUESTO I ES UN INHIBIDOR DE CISTEINA-PROTEASAS (CATEPSINA K) POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES RELACIONADAS CON UNA EXCESIVA DEGRADACION DE HUESO O CARTILAGO COMO OSTEOPOROSIS, PERIODONTITIS, ARTRITIS, ENFERMEDAD GINGIVAL O PERIODONTALREFERS TO ALCOXYPYRROLIDINONE COMPOUNDS OF FORMULA I, WHERE X IS O, S, SO, SO2; Y IS H2, O; R1 IS H, C1-C6 ALKYL, C2-C6 ALKENYL, (CH2) (0-6) CO2R ", PREFERRED GROUP a, b; R" IS H, C1-C6 ALKYL, C2-C6 ALKENYL, Ar-ALKYL C0-C6, AMONG OTHERS; R2 IS H, C1-C6 ALKYL, HET-C0-C6 ALKYL, PREFERRED ISOBUTYL, AMONG OTHERS; R3 IS H, C1-C6 ALKYL, C2-C6 ALKYL, C2-C6 ALKYNYL, PREFERRED GROUP c, d; Ar IS PHENYL, NAPHTHYL, OPTIONALLY SUBSTITUTED WITH Ph-ALKYL C0-C6, HET-ALKYL C0-C6, O (CH2) (1-6) NR`R ', AMONG OTHERS; R 'IS H, C1-C6 ALKYL, AMONG OTHERS; HET IS A 7-10 MEMBER HETERO CYCLIC BICYCLE RING, 5-7 MEMBER MONICYCLE RING OPTIONALLY SUBSTITUTED WITH OR ', N (R') 2, SR'CF3, AMONG OTHERS. PREFERRED COMPOUNDS ARE 3-BENZYLLOXY-1- (N-CARBOBENZYLOXY-L-LEUKINYL) PYRROLIDIN-4-ONA, 1- [2- (BENZYLOXYCARBONYLAMINE) -4-METHYLPENTIL] -3-BENZYLTHI-4-HYDROXYPYRROLIDINE, BETWEEN. IT ALSO REFERS TO A PROCEDURE TO CONVERT 3-BENZYLOXY-4-HYDROXY-1- (N-CARBOBENZYLOXY-L-LEUKINYL) PYRROLIDONE, AMONG OTHERS, INTO A COMPOUND OF FORMULA I. COMPOUND I IS A CYSTEIN PROTEIN-PROTEIN INHIBITOR K) SO IT MAY BE USEFUL FOR THE TREATMENT OF DISEASES RELATED TO EXCESSIVE DEGRADATION OF THE BONE OR CARTILAGE SUCH AS OSTEOPOROSIS, PERIODONTITIS, ARTHRITIS, GINGIVAL OR PERIODONTAL DISEASE
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8905698P | 1998-06-12 | 1998-06-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20000725A1 true PE20000725A1 (en) | 2000-09-28 |
Family
ID=22215426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1999000518A PE20000725A1 (en) | 1998-06-12 | 1999-06-11 | ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1086083A4 (en) |
| JP (1) | JP2002517485A (en) |
| AR (1) | AR018652A1 (en) |
| AU (1) | AU4564499A (en) |
| CA (1) | CA2334652A1 (en) |
| CO (1) | CO5040090A1 (en) |
| DZ (1) | DZ2815A1 (en) |
| MA (1) | MA24877A1 (en) |
| PE (1) | PE20000725A1 (en) |
| WO (1) | WO1999064399A1 (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030144175A1 (en) | 1998-12-23 | 2003-07-31 | Smithkline Beecham Corporation | Protease inhibitors |
| EP1232154A4 (en) | 1999-11-10 | 2004-06-23 | Smithkline Beecham Corp | Protease inhibitors |
| AU1474801A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| AU1588901A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| AU4344101A (en) | 2000-03-21 | 2001-10-03 | Smithkline Beecham Corp | Protease inhibitors |
| WO2002080920A1 (en) * | 2001-04-06 | 2002-10-17 | Axys Pharmaceuticals, Inc. | Arylacetamido-ketobenzoxazole as cysteine protease inhibitors |
| EP1465862A1 (en) | 2002-01-17 | 2004-10-13 | SmithKline Beecham Corporation | Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors |
| WO2009087379A2 (en) | 2008-01-09 | 2009-07-16 | Amura Therapeutics Limited | Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases |
| CN117940420A (en) | 2021-09-14 | 2024-04-26 | 勃林格殷格翰国际有限公司 | 3-Phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives and their use as pharmaceuticals |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0739204A4 (en) * | 1993-11-09 | 2000-03-15 | Merck & Co Inc | PIPERIDINES, PYRROLIDINES AND HEXAHYDRO-1H-AZEPINES PROMOTING THE RELEASE OF GROWTH HORMONE |
| US5770573A (en) * | 1993-12-06 | 1998-06-23 | Cytel Corporation | CS-1 peptidomimetics, compositions and methods of using the same |
| US5618792A (en) * | 1994-11-21 | 1997-04-08 | Cortech, Inc. | Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase |
-
1999
- 1999-06-09 DZ DZ990115A patent/DZ2815A1/en active
- 1999-06-10 MA MA25619A patent/MA24877A1/en unknown
- 1999-06-10 CO CO99036559A patent/CO5040090A1/en unknown
- 1999-06-10 AR ARP990102767A patent/AR018652A1/en unknown
- 1999-06-11 AU AU45644/99A patent/AU4564499A/en not_active Abandoned
- 1999-06-11 CA CA002334652A patent/CA2334652A1/en not_active Abandoned
- 1999-06-11 PE PE1999000518A patent/PE20000725A1/en not_active Application Discontinuation
- 1999-06-11 JP JP2000553408A patent/JP2002517485A/en not_active Withdrawn
- 1999-06-11 WO PCT/US1999/013334 patent/WO1999064399A1/en not_active Ceased
- 1999-06-11 EP EP99928614A patent/EP1086083A4/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| MA24877A1 (en) | 1999-12-31 |
| EP1086083A1 (en) | 2001-03-28 |
| CO5040090A1 (en) | 2001-05-29 |
| AR018652A1 (en) | 2001-11-28 |
| DZ2815A1 (en) | 2003-12-01 |
| WO1999064399A1 (en) | 1999-12-16 |
| AU4564499A (en) | 1999-12-30 |
| CA2334652A1 (en) | 1999-12-16 |
| EP1086083A4 (en) | 2001-09-26 |
| JP2002517485A (en) | 2002-06-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20001340A1 (en) | 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS | |
| PE20060777A1 (en) | INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES | |
| PE20010696A1 (en) | ADENOSINE A3 RECEPTOR AGONIST COMPOUNDS FOR THE TREATMENT OF ISCHEMIA | |
| PE2799A1 (en) | LACTAMS AND HETERO-CYCLIC IMIDES OF ARALQUILO AND ARALQUILIDENO | |
| PE71599A1 (en) | PROTEASE INHIBITORS | |
| EA200400815A1 (en) | CONTROLLED SYNTHESIS OF ZIPRAZIDONA AND ITS COMPOSITIONS | |
| BRPI0411268A (en) | process for the preparation of a substituted 3-aryl butyl amine compound | |
| IS6859A (en) | Crystalline form of atorvastatin | |
| CY1107228T1 (en) | Sodium channel blockers | |
| AR017236A1 (en) | BICYCLE COMPOUNDS [2.2.1] HEPTANS, PHARMACEUTICAL COMPOSITIONS, PROCEDURES TO TREAT | |
| PE20040672A1 (en) | DERIVATIVES OF PHENYL OR HETEROARYL AMINO ALKANE | |
| DK1140918T3 (en) | thrombin inhibitors | |
| EA200200819A1 (en) | CRYSTAL FORM II LINEZOLIDE | |
| EP1285655A4 (en) | STABILIZED PHARMACEUTICAL COMPOSITIONS CONTAINING CALCIUM CHANNEL BLOCKERS | |
| PE20000725A1 (en) | ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS | |
| BR0317005A (en) | Process for the preparation of optically pure active compounds | |
| PE20090548A1 (en) | AZA-BICYCLOHEXANE COMPOUNDS AS THROMBIN INHIBITORS | |
| IT1292437B1 (en) | ORTHO-METALLATION PROCESS USEFUL FOR THE SYNTHESIS OF 1 - TETRAZOL- 5-IL) 2-SUBSTITUTED BENZENES | |
| DK0657422T3 (en) | Naphthyloxyacetic acid derivatives such as PEG2 agonists and antagonists | |
| PE20040531A1 (en) | DERIVATIVES OF ISOINDOLONE, PREPARATION PROCESS, INTERMEDIATE COMPOUNDS OF THIS PROCESS AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM | |
| AR031356A1 (en) | LACTA MICO COMPOUND | |
| NO20002589D0 (en) | Bifenylamidinderivater | |
| DE60330758D1 (en) | CERTAIN PHARMACEUTICALLY VALUABLE SUBSTITUTED AMINO ALKYL HETEROCYCLES | |
| PE20011374A1 (en) | 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS | |
| DE69927044D1 (en) | PROCESS FOR RACEMICATION |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |