AR035714A1 - Pirazoles sustituidos y composiciones farmaceuticas que los contienen - Google Patents
Pirazoles sustituidos y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR035714A1 AR035714A1 ARP010103883A ARP010103883A AR035714A1 AR 035714 A1 AR035714 A1 AR 035714A1 AR P010103883 A ARP010103883 A AR P010103883A AR P010103883 A ARP010103883 A AR P010103883A AR 035714 A1 AR035714 A1 AR 035714A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocyclyl
- alkenyl
- phenyl
- hydrogen
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- 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
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- 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
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Pirazoles sustituidos de fórmula (1) o sales, ésteres o amidas farmacéuticamente aceptables de los mismos, en donde: R1 es hidrógeno, halógeno, alcoxi C1-5, hidroxi, alquilo C1-5, alquenilo C2-5, ciano, nitro R7R8N, acilo C2-8, R9OC=O, R10R11NC=O ó R10R11NSO2; o R1 es tomado conjuntamente con W como se describe más adelante; R2 es hidrógeno, halógeno, alcoxi C1-5, alquilo C1-5, alquenilo C2-5, haloalquilo C1-5, ciano o R48R49N; alternativamente, R1 y R2 pueden ser tomados en forma conjunta para formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros optativamente sustituido, anillo que puede ser insaturado o aromático; cada uno de R3 y R4 es independientemente hidrógeno o alquilo C1-5; cada uno de R5 y R6 es independientemente hidrógeno, alquilo C1-5, alquenilo C2-5, alcoxi C1-5, alquiltio C1-5, halógeno o un carbociclilo o heterociclilo de 4 a 7 miembros; alternativamente, R5 y R6 pueden ser tomados en forma conjunta para formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros optativamente sustituido, anillo que puede ser insaturado o aromático, y puede estar optativamente sustituido con entre uno y tres sustituyentes seleccionados independientemente entre halo, ciano, amino, nitro, R40, R40O-, R40S-, R40O(alquileno C1-5)-, R40O(C=O)-, R40(C=O)-, R40(C=S)-, R40(C=O)-O, R40O(C=O)(C=O), R40SO2, NHR62SO2- y NHR62(C=O)-; R40 es H, alquilo C1-5, alquenilo C2-5, fenilo, bencilo, fenetilo, heterociclilo C1-5, (heterociclil C1-5)alquileno C1-5, amino, o mono- o di(alquil C1-5)amino, ó R58OR59, en donde R58 es H, alquilo C1-5, alquenilo C2-5, fenilo, bencilo, fenetilo, heterociclilo C1-5 o (heterociclil C1-5)alquileno C1-6, y R59 es alquileno C1-5, fenileno, o heterociclilo C1-5 divalente; y R62 puede ser H además de los valores para R40; R7 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, naftilo, heterociclilo C1-5, acilo C2-8, aroilo, R27OC=O, R28R29NC=O, R27SO, R27SO2, ó R28R29NSO2; R8 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo o heterociclilo C1-5; alternativamente, R7 y R8 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; R9 es alquilo C1-5, fenilo, naftilo o heterociclilo C1-5; R21 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, naftilo, heterociclilo C1-5, acilo C2-8, aroilo, R30OC=O, R31R32NC=O, R30SO, R30SO2, ó R31R32NSO2; R22 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo o heterociclilo C1-5; alternativamente, R21 y R22 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; cada uno de R23, R26, R27, R30, R33, R44, R45 y R50 es alquilo C1-5, fenilo, naftilo o heterociclilo C1-5; R24 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, naftilo, heterociclilo C1-5, acilo C2-8, aroilo, R33OC=O, R34R35NC=O, R33SO, R33SO2 ó R34R35NSO2; R25 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo o heterociclilo C1-5; alternativamente, R24 y R25 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; cada uno de R10 y R11 es independientemente hidrógeno, alquilo C1-5, alquenilo C2-5, fenilo o heterociclilo C1-5; alternativamente, R10 y R11 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que pude ser saturado, insaturado o aromático; cada uno de R28, R29, R31, R32, R34, R35, R46, R47, R51 y R52 es independientemente hidrógeno, alquilo C1-5, fenilo o heterociclilo C1-5; alternativamente, R28 y R29, R31 y R32, R34 y R35, R46 y R47 ó R51 y R52, independientemente, pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; n es 1 ó 2; G representa alquenodiilo C3-6 o alcanodiilo C3-6, optativamente sustituido con hidroxi, halógeno, alquilo C1-5, alcoxi C1-5, oxo, hidroximino, CO2R60, R60R61NCO2, (L)-alquileno C1-4, (L)-alcoxi C1-5, N3 o [(L)-alquilen C1-5]amino; cada uno de R60 y R61 es independientemente hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, bencilo, fenetilo o heterociclilo C1-5; alternativamente R60 y R61, pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; L es amino, mono- o di-alquilamino C1-5, pirrolidinilo, morfolinilo, piperidinilo, homopiperidinilo, o piperazinilo donde los nitrógenos de anillos disponibles pueden ser optativamente sustituidos con alquilo C1-5, bencilo, acilo C2-5, alquilsulfonilo C2-5, o alquiloxicarbonilo C1-5; X es nitrógeno o R12C; Y es nitrógeno o R13C; Z es nitrógeno o R14C; R12 es hidrógeno, halógeno, alcoxi C1-5, alquilo C1-5, alquenilo C2-5, ciano, nitro, R21R22N, acilo C2-8, haloalquilo C1-5, heterociclilo C1-5, (heterociclilo C1-5)alquileno C1-5, R23OC=O, R23O(C=O)NH, R23SO, R22NHCO-, R22NH(C=O)NH-, R23(alquilen C1-4)NHCO-, R23SO2, ó R23SO2NH-; R13 es hidrógeno, halógeno, alcoxi C1-5, alquilo C1-5, alquenilo C2-5, ciano, nitro, R42R43N, acilo C2-8, haloalquilo C1-5, heterociclilo C1-5, (heterociclil C1-5)alquileno C1-5, R44OC=O, R44O(C=O)NH, R44SO, R43NHCO-, R43NH(C=O)NH-, R44(alquilen C1-4)NHCO-, R44SO2, ó R44SO2NH; R14 es hidrógeno, halógeno, alcoxi C1-5, alquilo C1-5, alquenilo C2-5, ciano, nitro, R24R25N, acilo C2-8, haloalquilo C1-5, heterociclilo C1-5, (heterociclil C1-5)alquileno C1-5, R26OC=O, R26O(C=O)NH, R26SO, R25NHCO-, R25NH(C=O)NH-, R26(alquilen C1-4)NHCO-, R26SO2, ó R26SO2NH; alternativamente, R12 y R13 ó R12 y R2 ó R13 y R14, pueden ser tomados en conjunto para formar un anillo carbocíclico o heterocíclico de 5 a 6 miembros optativamente sustituido, anillo que pude ser insaturado o aromático; Ar representa un anillo arilo o heteroarilo monocíclico o bicíclico, optativamente sustituido con entre 1 y 3 sustituyentes seleccionados entre halógeno, alcoxi C1-5, alquilo C1-5, alquenilo C2-5, ciano, nitro, R15R16N, R17SO2, R17S, R17SO, R17OC=O, R15R16NC=O, haloalquilo C1-5, haloalcoxi C1-5, haloalquiltio C1-5 y alquiltio C1-5; R15 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, bencilo, heterociclilo C1-5, acilo C2-8, aroilo, R53OC=O, R54R55NC=O, R53S, R53SO, R53SO2, ó R54R55NSO2; R16 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, bencilo o heterociclilo C1-5; alternativamente, R15 y R16 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros, optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; cada uno de R17 y R53 es alquilo C1-5, fenilo o heterociclilo C1-5; cada uno de R54 y R55 es independientemente hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, bencilo, o heterociclilo C1-5; alternativamente, R54 y R55 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; W representa SO2, C=O, CHR20, o un enlace covalente; o W y R1, tomados junto con el anillo de 6 miembros al cual están ambos unidos, forman una de las fórmulas (2) o (3), en donde Xa es O, S ó N; y Xb es O ó S; R20 es hidrógeno, alquilo C1-5, fenilo, bencilo, naftilo o heterociclilo C1-5; R42 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, naftilo, heterociclilo C1-5, acilo C2-8, aroilo, R45OC=O, R46R47NC=O, R45SO, R45SO2, ó R46R47NSO2; R43 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo o heterociclilo C1-5; alternativamente, R42 y R43 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; R44 es alquilo C1-5, alquenilo C2-5, fenilo, naftilo o heterociclilo C1-5; R48 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo, naftilo, heterociclilo C1-5, acilo C2-8, aroilo, R50OC=O, R51R52NC=O, R50SO, R50SO2, ó R51R52NSO2; R49 es hidrógeno, alquilo C1-5, alquenilo C3-5, fenilo o heterociclilo C1-5; alternativamente, R48 y R49 pueden ser tomados en conjunto para formar un anillo heterocíclico de 4 a 7 miembros optativamente sustituido, anillo que puede ser saturado, insaturado o aromático; y en donde cada uno de los grupos hidrocarbilo o heterocarbilo antes mencionados, a menos que se indique lo contrario y además de cualquier sustituyente especificado, es optativa e independientemente sustituido con entre 1 y 3 sustituyentes seleccionados entre metilo, halometilo hidroximetilo, halo, hidroxi, amino, nitro, ciano, alquilo C1-5, alcoxi C1-5, -COOH, acilo C2-6, [di(alquil C1-4)amino]alquileno C2-5, [di(alquil C1-4)amino]alquil C2-5-NH-CO- y haloalcoxi C1-5. Dichos compuestos son inhibidores de alta afinidad de la actividad proteolítica de la catepsina S humana y por lo tanto son útiles en la prevención, inhibición y tratamiento de trastornos mediados por dicha enzima, tal como lupus, artritis reumatoide y asma; y tienen utilidad potencial en la modulación de la respuesta inmune al transplante de tejido. Además, se dan a conocer composiciones farmacéuticas que los contienen.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22513800P | 2000-08-14 | 2000-08-14 | |
| US09/928,122 US7309703B2 (en) | 2000-08-14 | 2001-08-10 | Substituted pyrazoles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035714A1 true AR035714A1 (es) | 2004-07-07 |
Family
ID=26919335
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010103883A AR035714A1 (es) | 2000-08-14 | 2001-08-14 | Pirazoles sustituidos y composiciones farmaceuticas que los contienen |
Country Status (17)
| Country | Link |
|---|---|
| US (9) | US7309703B2 (es) |
| EP (1) | EP1309591B1 (es) |
| JP (1) | JP5140225B2 (es) |
| CN (1) | CN1329392C (es) |
| AR (1) | AR035714A1 (es) |
| AT (1) | ATE352552T1 (es) |
| AU (2) | AU2001281255B2 (es) |
| CA (1) | CA2419540A1 (es) |
| CY (1) | CY1106032T1 (es) |
| DE (1) | DE60126286T2 (es) |
| DK (1) | DK1309591T3 (es) |
| ES (1) | ES2281434T3 (es) |
| HK (1) | HK1052509B (es) |
| MX (1) | MXPA03001421A (es) |
| NZ (1) | NZ524193A (es) |
| PT (1) | PT1309591E (es) |
| WO (1) | WO2002014314A2 (es) |
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| GB0220214D0 (en) * | 2002-08-30 | 2002-10-09 | Novo Pharmaceuticals De Ltd | Compounds and their use |
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-
2001
- 2001-08-10 PT PT01959731T patent/PT1309591E/pt unknown
- 2001-08-10 AU AU2001281255A patent/AU2001281255B2/en not_active Expired
- 2001-08-10 ES ES01959731T patent/ES2281434T3/es not_active Expired - Lifetime
- 2001-08-10 MX MXPA03001421A patent/MXPA03001421A/es active IP Right Grant
- 2001-08-10 NZ NZ524193A patent/NZ524193A/xx unknown
- 2001-08-10 AT AT01959731T patent/ATE352552T1/de not_active IP Right Cessation
- 2001-08-10 DE DE60126286T patent/DE60126286T2/de not_active Expired - Lifetime
- 2001-08-10 CN CNB018170692A patent/CN1329392C/zh not_active Expired - Lifetime
- 2001-08-10 WO PCT/US2001/025289 patent/WO2002014314A2/en active IP Right Grant
- 2001-08-10 US US09/928,122 patent/US7309703B2/en not_active Expired - Lifetime
- 2001-08-10 JP JP2002519454A patent/JP5140225B2/ja not_active Expired - Lifetime
- 2001-08-10 CA CA002419540A patent/CA2419540A1/en not_active Abandoned
- 2001-08-10 AU AU8125501A patent/AU8125501A/xx active Pending
- 2001-08-10 EP EP01959731A patent/EP1309591B1/en not_active Expired - Lifetime
- 2001-08-10 DK DK01959731T patent/DK1309591T3/da active
- 2001-08-10 US US11/517,062 patent/US7589202B2/en not_active Expired - Lifetime
- 2001-08-14 AR ARP010103883A patent/AR035714A1/es unknown
-
2003
- 2003-07-04 HK HK03104770.5A patent/HK1052509B/zh not_active IP Right Cessation
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2006
- 2006-09-07 US US11/517,171 patent/US7388011B2/en not_active Expired - Lifetime
- 2006-09-07 US US11/517,518 patent/US7429591B2/en not_active Expired - Lifetime
- 2006-09-07 US US11/517,145 patent/US7417046B2/en not_active Expired - Lifetime
- 2006-09-07 US US11/517,040 patent/US7452890B2/en not_active Expired - Lifetime
- 2006-09-07 US US11/517,212 patent/US7393850B2/en not_active Expired - Lifetime
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2007
- 2007-02-20 CY CY20071100223T patent/CY1106032T1/el unknown
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- 2008-07-24 US US12/220,539 patent/US7772236B2/en not_active Expired - Fee Related
- 2008-07-24 US US12/220,516 patent/US20080300255A1/en not_active Abandoned
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