CO5040090A1 - Inhibidores de proteasas - Google Patents
Inhibidores de proteasasInfo
- Publication number
- CO5040090A1 CO5040090A1 CO99036559A CO99036559A CO5040090A1 CO 5040090 A1 CO5040090 A1 CO 5040090A1 CO 99036559 A CO99036559 A CO 99036559A CO 99036559 A CO99036559 A CO 99036559A CO 5040090 A1 CO5040090 A1 CO 5040090A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- group
- cycloalkyl
- het
- alkynyl
- Prior art date
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-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
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- PMPVIKIVABFJJI-UHFFFAOYSA-N Cyclobutane Chemical compound C1CCC1 PMPVIKIVABFJJI-UHFFFAOYSA-N 0.000 abstract 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-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
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical class [H]C1([H])C([H])([H])C1([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
- 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
- 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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
Un compuesto según la fórmula (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 U es O, entonces el enlace ------ representa un enlace doble;R1 se selecciona del grupo formado por hidrógeno,alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo CO -C6 , Het-alquilo C0 -C6 , (CH2 )0-6 CO2 R", y (CH2 )O-6 Ar;R" se selecciona del grupo formado por hidrógeno,alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo C0 -C6 y Het-alquilo C0 -C6 ;R2 se selecciona del grupo formado por H, alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo CO -C6 , Ar-alquilo CO -C6 y Het-alquilo CO -C6 ;R3 se selecciona del grupo formado por H, alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo C0 -C6 y Het-alquilo CO -C6 ;alquilo C1 -C6 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, y los isomeros alifáticos de los mismos; cicloalquilo C3 -C6 se selecciona del grupo formado por ciclopropano, ciclobutano, ciclopentano y ciclohexano sustituidos y no sustituidos; ...
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8905698P | 1998-06-12 | 1998-06-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5040090A1 true CO5040090A1 (es) | 2001-05-29 |
Family
ID=22215426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO99036559A CO5040090A1 (es) | 1998-06-12 | 1999-06-10 | Inhibidores de proteasas |
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 |
| AU1474801A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| EP1232154A4 (en) | 1999-11-10 | 2004-06-23 | Smithkline Beecham Corp | PROTEASE INHIBITORS |
| US6596715B1 (en) | 1999-11-10 | 2003-07-22 | Smithkline Beecham Corporation | Protease inhibitors |
| EA005893B1 (ru) | 2000-03-21 | 2005-06-30 | Смитклайн Бичам Корпорейшн | Ингибиторы протеаз |
| US20020156063A1 (en) * | 2001-04-06 | 2002-10-24 | Setti Eduardo L. | Arylacetamido-ketobenzoxazole as cysteine protease inhibitors |
| WO2003062192A1 (en) | 2002-01-17 | 2003-07-31 | Smithkline Beecham Corporation | Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors |
| EP2719700A1 (en) | 2008-01-09 | 2014-04-16 | Amura Therapeutics Limited | Tetrahydrofuro(3,2-b)pyrrol-3-one derivatives as inhibitors of cysteine proteinases |
| US12115157B2 (en) | 2021-09-14 | 2024-10-15 | Boehringer Ingelheim International Gmbh | 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives and the use thereof as medicament |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR960705808A (ko) * | 1993-11-09 | 1996-11-08 | 조셉 에프. 디프리마 | 성장 호르몬의 방출을 촉진시키는 피페리딘, 피롤리딘 및 헥사하이드로-1H-아제핀(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 AR ARP990102767A patent/AR018652A1/es unknown
- 1999-06-10 CO CO99036559A patent/CO5040090A1/es unknown
- 1999-06-10 MA MA25619A patent/MA24877A1/fr unknown
- 1999-06-11 PE PE1999000518A patent/PE20000725A1/es not_active Application Discontinuation
- 1999-06-11 JP JP2000553408A patent/JP2002517485A/ja not_active Withdrawn
- 1999-06-11 EP EP99928614A patent/EP1086083A4/en not_active Withdrawn
- 1999-06-11 CA CA002334652A patent/CA2334652A1/en not_active Abandoned
- 1999-06-11 AU AU45644/99A patent/AU4564499A/en not_active Abandoned
- 1999-06-11 WO PCT/US1999/013334 patent/WO1999064399A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| CA2334652A1 (en) | 1999-12-16 |
| AR018652A1 (es) | 2001-11-28 |
| WO1999064399A1 (en) | 1999-12-16 |
| EP1086083A4 (en) | 2001-09-26 |
| MA24877A1 (fr) | 1999-12-31 |
| EP1086083A1 (en) | 2001-03-28 |
| JP2002517485A (ja) | 2002-06-18 |
| PE20000725A1 (es) | 2000-09-28 |
| DZ2815A1 (fr) | 2003-12-01 |
| AU4564499A (en) | 1999-12-30 |
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