CO5280093A1 - TREATMENT METHODS - Google Patents
TREATMENT METHODSInfo
- Publication number
- CO5280093A1 CO5280093A1 CO01029288A CO01029288A CO5280093A1 CO 5280093 A1 CO5280093 A1 CO 5280093A1 CO 01029288 A CO01029288 A CO 01029288A CO 01029288 A CO01029288 A CO 01029288A CO 5280093 A1 CO5280093 A1 CO 5280093A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- group
- het
- cycloalkyl
- alkynyl
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 41
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 13
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 102200160920 rs35304565 Human genes 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 102000004172 Cathepsin L Human genes 0.000 abstract 1
- 108090000624 Cathepsin L Proteins 0.000 abstract 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un método para inhibir la catepsina L, que comprende administrar, a un paciente que lo necesite, una cantidad eficaz de un compuesto de Fórmula I: <EMI FILE="01029288_1" ID="1" IMF=JPEG >en la que:R1 seleccionado del grupo que consiste en:<EMI FILE="01029288_2" ID="2" IMF=JPEG > R2 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6 -alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R9C(O)-, R9C(S)-, R9SO2-, R9OC(O)-, R9R11NC(O)-,R9R11NC(S)-, R9(R11)NSO2-, R3 es seleccionado del grupo que consiste en: H, alquilo Cl-6, cicloalquil C3-6-alquilo C0-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6, y Ar-alquilo C0-6;R3 y R' pueden estar unidos para formar un anillo de pirrolidina, piperidina o morfolina;R4 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R5C(O)-, R5C(S)-, R5SO2-, R5OC(O), R5R13NC(O)-, y R5R13NC(S)-; - 2 -R5 es seleccionado del grupo que consiste en: 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; R6 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6 alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R7 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R10C(O)-, R10C(S)-, - R10SO2-, R10OC(O)-, R10R14N-C(O)-, y R10 R14NC(S)-;R8 es seleccionado del grupo que consiste en: H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6 y Ar-alquilo C0-6; R9 es seleccionado del grupo que consiste en: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6, R10 seleccionado del grupo que consiste en: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R11 es seleccionado del grupo que consiste en: H, alquilo C1-6 Ar-alquilo C0-6 y Het-alquilo C0-6; R12 es seleccionado del grupo que consiste en: H, alquilo Cl-6 Ar-alquilo C0-6 y Het-alquilo C0-6, R13 es seleccionado del grupo que consiste en: H, alquilo C1-6 Ar-alquilo C0-6 y Het-alquilo C0-6; R14 es seleccionado del grupo que consiste en: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6;R´ es seleccionado del grupo que consiste en: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R" es seleccionado del grupo que consiste en: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6, R"' es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; X es seleccionado del grupo que consiste en: CH2, S y O; yZ es seleccionado del grupo que consiste en: C(O) y CH2; y sales, hidratos y solvatos farmacéuticamente aceptables del mismo.A method for inhibiting cathepsin L, which comprises administering, to a patient in need, an effective amount of a compound of Formula I: <EMI FILE = "01029288_1" ID = "1" MFI = JPEG> in which: R1 selected from the group consisting of: <EMI FILE = "01029288_2" ID = "2" MFI = JPEG> R2 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar -C0-6 alkyl, Het-C0-6 alkyl, R9C (O) -, R9C (S) -, R9SO2-, R9OC (O) -, R9R11NC (O) -, R9R11NC (S) -, R9 (R11) NSO2-, R3 is selected from the group consisting of: H, Cl-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Het-C0-6 alkyl, and Ar-alkyl C0-6; R3 and R 'may be linked to form a pyrrolidine, piperidine or morpholine ring; R4 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar- C0-6 alkyl, Het-C0-6 alkyl, R5C (O) -, R5C (S) -, R5SO2-, R5OC (O), R5R13NC (O) -, and R5R13NC (S) -; - 2 -R5 is selected from the group consisting of: H, C1-6 alkyl C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0 alkyl -6; R6 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R7 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R10C (O) -, R10C (S) -, - R10SO2-, R10OC (O) -, R10R14N-C (O) -, and R10 R14NC (S) -; R8 is selected from the group consisting of: H, C1-6 alkyl, C2-6 alkenyl, alkynyl C2-6, Het-C0-6 alkyl and Ar-C0-6 alkyl; R9 is selected from the group consisting of: C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R10 selected from the group consisting of: C1-6 alkyl , C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R11 is selected from the group consisting of: H, C1-6 alkyl Ar-C0-6 alkyl and Het-C0-6 alkyl; R12 is selected from the group consisting of: H, Cl-6 alkyl Ar-C0-6 alkyl and Het-C0-6 alkyl, R13 is selected from the group consisting of: H, C1-6 alkyl Ar-C0-6 alkyl and Het-C0-6 alkyl; R14 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R 'is selected from the group consisting of: H, C1-6 alkyl, Ar-alkyl C0-6 and Het-C0-6 alkyl; R "is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R" 'is selected from the group consisting of: H, C1-6 alkyl, cycloalkyl C3-6-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; X is selected from the group consisting of: CH2, S and O; and Z is selected from the group consisting of: C (O) and CH2; and pharmaceutically acceptable salts, hydrates and solvates thereof.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19771700P | 2000-04-18 | 2000-04-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5280093A1 true CO5280093A1 (en) | 2003-05-30 |
Family
ID=22730469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO01029288A CO5280093A1 (en) | 2000-04-18 | 2001-04-16 | TREATMENT METHODS |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1303281A4 (en) |
| JP (1) | JP2003531122A (en) |
| AU (1) | AU2001253560A1 (en) |
| CO (1) | CO5280093A1 (en) |
| WO (1) | WO2001078734A1 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004527575A (en) * | 2001-05-17 | 2004-09-09 | スミスクライン・ビーチャム・コーポレイション | Protease inhibitor |
| EP1551823A1 (en) * | 2002-10-08 | 2005-07-13 | Merck Frosst Canada Inc. | 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis |
| WO2009087379A2 (en) | 2008-01-09 | 2009-07-16 | Amura Therapeutics Limited | Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0104768A3 (en) * | 1998-12-23 | 2002-05-28 | Smithkline Beecham Corp | 4-amino-3-oxo-azepanes as protease inhibitors and pharmaceutical compositions containing the same |
| AU1474601A (en) * | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| US6534498B1 (en) * | 1999-11-10 | 2003-03-18 | Smithkline Beecham Corporation | Protease inhibitors |
| EP1235577A4 (en) * | 1999-11-10 | 2003-04-09 | Smithkline Beecham Corp | Protease inhibitors |
| WO2001034158A1 (en) * | 1999-11-10 | 2001-05-17 | Smithkline Beecham Corporation | Protease inhibitors |
| EP1229912A4 (en) * | 1999-11-10 | 2003-05-07 | Smithkline Beecham Corp | Protease inhibitors |
| WO2001034160A1 (en) * | 1999-11-10 | 2001-05-17 | Smithkline Beecham Corporation | Protease inhibitors |
| AU1474701A (en) * | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| CA2404206A1 (en) * | 2000-03-21 | 2001-09-27 | Smithkline Beecham Corporation | Protease inhibitors |
-
2001
- 2001-04-16 CO CO01029288A patent/CO5280093A1/en not_active Application Discontinuation
- 2001-04-17 AU AU2001253560A patent/AU2001253560A1/en not_active Abandoned
- 2001-04-17 EP EP01927076A patent/EP1303281A4/en not_active Withdrawn
- 2001-04-17 WO PCT/US2001/012386 patent/WO2001078734A1/en not_active Application Discontinuation
- 2001-04-17 JP JP2001576034A patent/JP2003531122A/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP2003531122A (en) | 2003-10-21 |
| EP1303281A4 (en) | 2006-02-15 |
| EP1303281A1 (en) | 2003-04-23 |
| WO2001078734A1 (en) | 2001-10-25 |
| AU2001253560A1 (en) | 2001-10-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |