AR034278A1 - COMPOUNDS OF 4-AMINO-AZEPAN-3-ONA 1-AMINO-1-ACIL CYCLALCANO C3-6 REPLACED, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, INTERMEDIARIES, PROCEDURE FOR THE SYNTHESIS OF SUCH COMPOUNDS, AND THE USE OF SUCH COMPOSITIONS MEDICINES - Google Patents
COMPOUNDS OF 4-AMINO-AZEPAN-3-ONA 1-AMINO-1-ACIL CYCLALCANO C3-6 REPLACED, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, INTERMEDIARIES, PROCEDURE FOR THE SYNTHESIS OF SUCH COMPOUNDS, AND THE USE OF SUCH COMPOSITIONS MEDICINESInfo
- Publication number
- AR034278A1 AR034278A1 ARP010105409A ARP010105409A AR034278A1 AR 034278 A1 AR034278 A1 AR 034278A1 AR P010105409 A ARP010105409 A AR P010105409A AR P010105409 A ARP010105409 A AR P010105409A AR 034278 A1 AR034278 A1 AR 034278A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het
- compounds
- cycloalkyl
- amino
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
-
- 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
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Compuestos de 4-amino-azepan-3-ona 1-amino-1-acil cicloalcano C3-6 sustituidos de Fórmula (1), en la que: R1 es un compuesto de la fórmula (2); R2 se selecciona del grupo formado por: 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-, R9SO2R11N(CO)-, un resto de fórmula (3), (4) y (5); R4 se selecciona del grupo formado por: 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)-, R5R12NC(O)-, y R5R12NC(S)-; R5 se selecciona entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, alcanoil C3-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R6 es H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R7 se selecciona del grupo formado por: 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)-, R10R13NC(O)-, y R10R13NC(S)-; R8 se selecciona entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6 y Ar-alquilo C0-6; R9 se selecciona del grupo formado por: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, -Ar-COOH, y Het-alquilo C0-6; R10 es alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R11, R12, R13, R' y R'' independientemente uno de otro son: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R''' se selecciona de entre H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; Z es C(O) ó CH2; y n es un número entreo de 1 a 5; y sus sales, hidratos y solvatos farmacéuticamente aceptables. Dichos compuestos son inhibidores de proteasas, más particularmente de la catepsina K, y son útiles para tratar enfermedades en las que están implicadas cisteína-proteasas, especialmente enfermedades de excesiva pérdida de masa ósea o cartilaginosa o degradación de matriz, por ejemplo osteoporosis, enfermedad gingival, artritis, enfermedad de Paget, hipelcalcemia de tumores malignos, y enfermedad metabólica de los huesos. También se dan a conocer: composiciones farmacéuticas que comprenden dichos compuestos, intermediarios útiles para la síntesis de dichos compuestos, un procedimiento para la síntesis de dichos compuestos, y el uso de dichos compuestos en la fabricación de medicamentos.Substituted 4-amino-azepan-3-one 1-amino-1-acyl cycloalkane C3-6 compounds of Formula (1), wherein: R1 is a compound of the formula (2); 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-, R9SO2R11N (CO) -, a remainder of formula (3), (4) and (5) ; 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) -, R5R12NC (O) -, and R5R12NC (S) -; R5 is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl-C0-6 alkyl, C3-6 alkanoyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl ; R6 is H, C1-6 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) -, R10R13NC (O) -, and R10R13NC (S) -; R8 is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, 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, -Ar-COOH, and Het-C0-6 alkyl; R10 is C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R11, R12, R13, R 'and R' 'independently of one another are: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R '' 'is selected from H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; Z is C (O) or CH2; and n is a number between 1 and 5; and its pharmaceutically acceptable salts, hydrates and solvates. Such compounds are protease inhibitors, more particularly cathepsin K, and are useful for treating diseases in which cysteine proteases are involved, especially diseases of excessive bone or cartilage mass loss or matrix degradation, for example osteoporosis, gingival disease. , arthritis, Paget's disease, malignant tumor hypelcalcemia, and metabolic bone disease. Also disclosed are: pharmaceutical compositions comprising said compounds, intermediates useful for the synthesis of said compounds, a process for the synthesis of said compounds, and the use of said compounds in the manufacture of medicaments.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25250800P | 2000-11-22 | 2000-11-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR034278A1 true AR034278A1 (en) | 2004-02-18 |
Family
ID=22956303
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010105409A AR034278A1 (en) | 2000-11-22 | 2001-11-20 | COMPOUNDS OF 4-AMINO-AZEPAN-3-ONA 1-AMINO-1-ACIL CYCLALCANO C3-6 REPLACED, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, INTERMEDIARIES, PROCEDURE FOR THE SYNTHESIS OF SUCH COMPOUNDS, AND THE USE OF SUCH COMPOSITIONS MEDICINES |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP1392657A4 (en) |
| JP (1) | JP2005513083A (en) |
| KR (1) | KR20040004445A (en) |
| CN (1) | CN1635903A (en) |
| AR (1) | AR034278A1 (en) |
| AU (1) | AU2001298052A1 (en) |
| BR (1) | BR0115473A (en) |
| CA (1) | CA2436850A1 (en) |
| CZ (1) | CZ20031403A3 (en) |
| HU (1) | HUP0301964A3 (en) |
| IL (1) | IL155997A0 (en) |
| MX (1) | MXPA03004542A (en) |
| NO (1) | NO20032328L (en) |
| PL (1) | PL366232A1 (en) |
| UY (1) | UY27032A1 (en) |
| WO (1) | WO2003053331A2 (en) |
| ZA (1) | ZA200303848B (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030144175A1 (en) | 1998-12-23 | 2003-07-31 | Smithkline Beecham Corporation | Protease inhibitors |
| NZ520588A (en) | 2000-03-21 | 2004-06-25 | Smithkline Beecham Corp | Protease inhibitors |
| WO2001095911A1 (en) * | 2000-06-14 | 2001-12-20 | Smithkline Beecham Corporation | Protease inhibitors |
| KR20100023948A (en) | 2007-06-08 | 2010-03-04 | 닛뽕 케미파 가부시키가이샤 | Therapeutic or prophylactic agent for cerebral aneurysm |
| WO2009054454A1 (en) | 2007-10-24 | 2009-04-30 | National University Corporation Tokyo Medical And Dental University | Regulator for signaling of toll-like receptor, which comprises cathepsin inhibitor as active ingredient |
Family Cites Families (3)
| 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 |
| NZ520588A (en) * | 2000-03-21 | 2004-06-25 | Smithkline Beecham Corp | Protease inhibitors |
| WO2001095911A1 (en) * | 2000-06-14 | 2001-12-20 | Smithkline Beecham Corporation | Protease inhibitors |
-
2001
- 2001-11-19 HU HU0301964A patent/HUP0301964A3/en unknown
- 2001-11-19 CZ CZ20031403A patent/CZ20031403A3/en unknown
- 2001-11-19 PL PL01366232A patent/PL366232A1/en not_active Application Discontinuation
- 2001-11-19 JP JP2003554091A patent/JP2005513083A/en not_active Withdrawn
- 2001-11-19 IL IL15599701A patent/IL155997A0/en unknown
- 2001-11-19 BR BR0115473-7A patent/BR0115473A/en not_active Application Discontinuation
- 2001-11-19 WO PCT/US2001/051647 patent/WO2003053331A2/en not_active Application Discontinuation
- 2001-11-19 MX MXPA03004542A patent/MXPA03004542A/en unknown
- 2001-11-19 KR KR10-2003-7006807A patent/KR20040004445A/en not_active Application Discontinuation
- 2001-11-19 CN CNA018220533A patent/CN1635903A/en active Pending
- 2001-11-19 EP EP01275089A patent/EP1392657A4/en not_active Withdrawn
- 2001-11-19 CA CA002436850A patent/CA2436850A1/en not_active Abandoned
- 2001-11-19 AU AU2001298052A patent/AU2001298052A1/en not_active Abandoned
- 2001-11-20 AR ARP010105409A patent/AR034278A1/en unknown
- 2001-11-21 UY UY27032A patent/UY27032A1/en not_active Application Discontinuation
-
2003
- 2003-05-16 ZA ZA200303848A patent/ZA200303848B/en unknown
- 2003-05-22 NO NO20032328A patent/NO20032328L/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA03004542A (en) | 2003-09-10 |
| NO20032328D0 (en) | 2003-05-22 |
| EP1392657A2 (en) | 2004-03-03 |
| KR20040004445A (en) | 2004-01-13 |
| EP1392657A4 (en) | 2004-03-10 |
| CZ20031403A3 (en) | 2003-10-15 |
| HUP0301964A3 (en) | 2007-09-28 |
| UY27032A1 (en) | 2002-07-31 |
| BR0115473A (en) | 2004-09-28 |
| WO2003053331A2 (en) | 2003-07-03 |
| NO20032328L (en) | 2003-07-02 |
| CN1635903A (en) | 2005-07-06 |
| CA2436850A1 (en) | 2003-07-03 |
| AU2001298052A1 (en) | 2003-07-09 |
| ZA200303848B (en) | 2004-06-28 |
| HUP0301964A2 (en) | 2007-02-28 |
| IL155997A0 (en) | 2003-12-23 |
| PL366232A1 (en) | 2005-01-24 |
| WO2003053331A3 (en) | 2003-11-13 |
| JP2005513083A (en) | 2005-05-12 |
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