AR018652A1 - Inhibidor de catepsina k del tipo pirrolidinona, composicion farmaceuticamente eficaz, usos de dichos compuestos para preparar medicamentos, yprocedimiento para producir dichos inhibidores - Google Patents
Inhibidor de catepsina k del tipo pirrolidinona, composicion farmaceuticamente eficaz, usos de dichos compuestos para preparar medicamentos, yprocedimiento para producir dichos inhibidoresInfo
- Publication number
- AR018652A1 AR018652A1 ARP990102767A ARP990102767A AR018652A1 AR 018652 A1 AR018652 A1 AR 018652A1 AR P990102767 A ARP990102767 A AR P990102767A AR P990102767 A ARP990102767 A AR P990102767A AR 018652 A1 AR018652 A1 AR 018652A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- carbon
- het
- substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 2
- 150000001875 compounds Chemical class 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 16
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 5
- 239000011203 carbon fibre reinforced carbon Substances 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000001624 naphthyl group Chemical group 0.000 abstract 3
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 229940122156 Cathepsin K inhibitor Drugs 0.000 abstract 1
- PMPVIKIVABFJJI-UHFFFAOYSA-N Cyclobutane Chemical compound C1CCC1 PMPVIKIVABFJJI-UHFFFAOYSA-N 0.000 abstract 1
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical class [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 abstract 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 abstract 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 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)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
Abstract
Inhibidor de catepsina K del tipo pirrolidinona que tiene la formula (I), en la que: X se selecciona del grupo formado por oxígeno, azufre, SO y SO2;Y se selecciona del grupo formado por H2 y oxígeno; donde, si Y es H2, entonces el enlace - - - - representa dos enlaces sencillos y donde si Y es O,entones el enlace - - - - representa un enlace doble; R1 se selecciona del grupo formado por hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6,cicloalquilC3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, (CH2)0-6CO2R, y (CH2)0-6Ar; R11 se selecciona del grupo formado por hidrogeno, alquilo C1-6,alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R2 se selecciona del grupo formado por H, alquilo C1-6,alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R3 se selecciona del grupo formado por H, alquilo C1-6,alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; alquilo C1-6 se selecciona del grupo formado pormetilo, etilo, n-propilo, isopropilo, n-butilo, isobutilo, t-butilo, pentilo, n-pentilo, isopentilo, neopentilo y hexilo sustituidos o no sustituidos, ylos isomeros alifáticos de los mismos;cicloalquilo C3-6 se selecciona del grupo formado por ciclopropano, ciclobutano, ciclopentano, y ciclohexanosustituidos y no sustituidos; alquenilo C2-6 es un grupo alquilo C2-6, en el que se ha sustituido un enlace sencillo carbono-carbono por un dobleenlace carbono-carbono; alquinilo C2-6 es un grupo alquilo C2-6, en el que se ha sustituido un enlace sencillo carbono-carbono por un triple enlacecarbono-carbono; Ar se selecciona del grupo formado por fenilo o naftilo; o fenilo o naftilo sustituido con uno o más de Ph-alquilo C0-6, Het-alquiloC0-6, alcoxi C1-6, Ph-alcoxi C0-6, Het-alcoxi C0-6, OH, (CH2)0-6CO2R, donde R es como se ha definido anteriormente, (CH2)1-6NRR, O(CH2)1-6NRR; ofenilo o naftilo sustituido con 1-3 restos seleccionadosentre alquilo C1-4, OR, N(R)2, SR, CF3, NO2, CN, CO2R, CON(R), F, Cl, Br e I, o sustituido
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8905698P | 1998-06-12 | 1998-06-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR018652A1 true AR018652A1 (es) | 2001-11-28 |
Family
ID=22215426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990102767A AR018652A1 (es) | 1998-06-12 | 1999-06-10 | Inhibidor de catepsina k del tipo pirrolidinona, composicion farmaceuticamente eficaz, usos de dichos compuestos para preparar medicamentos, yprocedimiento para producir dichos inhibidores |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1086083A4 (es) |
| JP (1) | JP2002517485A (es) |
| AR (1) | AR018652A1 (es) |
| AU (1) | AU4564499A (es) |
| CA (1) | CA2334652A1 (es) |
| CO (1) | CO5040090A1 (es) |
| DZ (1) | DZ2815A1 (es) |
| MA (1) | MA24877A1 (es) |
| PE (1) | PE20000725A1 (es) |
| WO (1) | WO1999064399A1 (es) |
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 |
| US6534498B1 (en) | 1999-11-10 | 2003-03-18 | Smithkline Beecham Corporation | Protease inhibitors |
| AU1588901A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| US6583137B1 (en) | 1999-11-10 | 2003-06-24 | Smithkline Beecham Corporation | Protease inhibitors |
| OA12323A (en) | 2000-03-21 | 2006-05-15 | Smithkline Beecham Corp | Protease inhibitors. |
| US20020156063A1 (en) * | 2001-04-06 | 2002-10-24 | Setti Eduardo L. | Arylacetamido-ketobenzoxazole as cysteine protease inhibitors |
| JP2005515254A (ja) | 2002-01-17 | 2005-05-26 | スミスクライン ビーチャム コーポレーション | カテプシンｋ阻害剤として有用なシクロアルキルケトアミド誘導体 |
| 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 (zh) | 2021-09-14 | 2024-04-26 | 勃林格殷格翰国际有限公司 | 3-苯氧基氮杂环丁烷-1-基-杂芳基吡咯烷衍生物及其作为药物的用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995013069A1 (en) * | 1993-11-09 | 1995-05-18 | Merck & Co., Inc. | Piperidines, pyrrolidines and hexahydro-1h-azepines promote 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/xx active
- 1999-06-10 CO CO99036559A patent/CO5040090A1/es unknown
- 1999-06-10 AR ARP990102767A patent/AR018652A1/es unknown
- 1999-06-10 MA MA25619A patent/MA24877A1/fr unknown
- 1999-06-11 CA CA002334652A patent/CA2334652A1/en not_active Abandoned
- 1999-06-11 JP JP2000553408A patent/JP2002517485A/ja not_active Withdrawn
- 1999-06-11 AU AU45644/99A patent/AU4564499A/en not_active Abandoned
- 1999-06-11 PE PE1999000518A patent/PE20000725A1/es not_active Application Discontinuation
- 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 |
|---|---|
| AU4564499A (en) | 1999-12-30 |
| EP1086083A4 (en) | 2001-09-26 |
| EP1086083A1 (en) | 2001-03-28 |
| DZ2815A1 (fr) | 2003-12-01 |
| WO1999064399A1 (en) | 1999-12-16 |
| PE20000725A1 (es) | 2000-09-28 |
| CO5040090A1 (es) | 2001-05-29 |
| JP2002517485A (ja) | 2002-06-18 |
| CA2334652A1 (en) | 1999-12-16 |
| MA24877A1 (fr) | 1999-12-31 |
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