AR058614A1 - Compuesto de azaindol , composicion que lo comprende y su uso para preparar un medicamento - Google Patents
Compuesto de azaindol , composicion que lo comprende y su uso para preparar un medicamentoInfo
- Publication number
- AR058614A1 AR058614A1 ARP060105721A ARP060105721A AR058614A1 AR 058614 A1 AR058614 A1 AR 058614A1 AR P060105721 A ARP060105721 A AR P060105721A AR P060105721 A ARP060105721 A AR P060105721A AR 058614 A1 AR058614 A1 AR 058614A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- independently
- haloalkyl
- hydroxyalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 13
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 7
- 125000001475 halogen functional group Chemical group 0.000 abstract 7
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- -1 azaindole compound Chemical class 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004849 alkoxymethyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000012634 fragment Substances 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Composicion que comprende dicho compuesto y su uso para preparar un medicamento util para el tratamiento del cáncer. Reivindicacion 1: Un compuesto de azaindol caracterizado porque es de formula (1) o una sal farmacéuticamente aceptable del mismo, donde el resto de formula (2) representa un fragmento de anillo heteroaromático de 5 miembros; A es >C=Y o >S(O)x donde Y es O, S o N-R1; donde x es 1 o 2; R1 es independientemente H, alquilo C1-3, o ciclopropilo; R2 es H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, hidroxialquilo C1-6, aminoalquilo C1-6, alcoximetilo C1-6, hidroxi, -(CH2)y-Ar-(R7)z, o NR8R9, con la condicion de que cuando A es S(O)x, R2 no sea H; donde y es 0, 1 o 2; y z es un numero entero no negativo no mayor que el numero de posiciones disponibles sobre Ar para sustitucion; Ar es fenilo o heteroarilo; R3 es independientemente H, alquilo C1-6, alquenilo C2-6, haloalquilo C1-6, hidroxialquilo C1-6, aminoalquilo C1-6, alquilamino C1-6-alquilo C1-6, dialquilamino C1-6-alquilo C1-6, -(CH2)w-R10; donde w es 1 o 2; R4 es independientemente alquilo C1-6, halo, haloalquilo C1-6, o Ar-(R7)z, R5 es independientemente alquilo C1-6, halo, haloalquilo C1-6, Ar-(R7)z, -(CH2)aNR13R14, Ar-(CH2)aNR13R14, -A'- NR1-(CH2)b-Aö, -CH2CH2C(O)-A'ö, o -Ar'-(C(O)(CH2)aNR13R14)c; donde A' es C(O) o CH2; Aö es H, NR13R14, tioalquilo C1-6, alcoxi C1-6, -SO2CH3, o -OH; A'ö es -OH, alcoxi C1-6, -NR13R14; y Ar' es un anillo heterocicloalquilo de 5 o 6 miembros donde a es independientemente 0, 1 o 2; b es 1, 2 o 3, con la condicion de que cuando b es 1, Aö sea H, y c es 0 o 1; cada uno de R6 y R7 es independientemente halo, ciano, nitro, alquilo C1-6, COOH, alquilcarbonilo C1-6, alquilcarbonil C1-6-alquilo C1-, amino, alquilamino C1-6, dialquilamino C1-6, aminoalquilo C1-6, alquilamino C1-6-alquilo C1-6, dialquilamino C1-6-alquilo C1-6, OH, haloalquilo C1-6, hidroxialquilo C1-6, alcoxi C1-6, alcoxi C1-6-alquilo C1-6, heteroarilo, o fenilo; R8 es H o alquilo C1-6; R9 es H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, -(CH2)y-Ar-(R7)z; o R8 y R9, junto con el átomo de N al que están unidos forman un anillo heterocicloalquilo de 5 o 6 miembros opcionalmente sustituido con alquilo C1-6, halo, amino, ciano, alcoxi C1-6, o OH; R10 es heterocicloalquilo, Ar-(R7)z, COOH, o C(O)-NR11R12; R11 es H o alquilo C1-3; R12 es H, alquilo C1-6, haloalilo C1-3, o hidroxialquilo C1-3; o R11 y R12 junto con el átomo de N al que están unidos forman un anillo heterocicloalquilo de 5 o 6 miembros opcionalmente sustituido con alquilo C1-6, halo, amino, ciano, alcoxi C1-6, o hidroxi; R13 es H, alquilo C1-6, o hidroxialquilo C1-6; R14 es H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, alquilamino C1-6, o SO2CH3; o R13 y R14, junto con el átomo de N al que están unidos forman un anillo heterocicloalquilo de 5 o 6 miembros opcionalmente sustituido con alquilo C1-6, halo, amino, ciano, alcoxi C1-6, hidroxialquilo C1-6, o OH; y cada uno de R15 y R16 es independientemente H, alquilo C1-6, o halo, o R15 y R16, junto con el átomo de C al que están unidos forman ciclopropilo, C=O, C=S, o C=NR1; m es 0 o 1; cada uno de n, o, y q es independientemente 0, 1 o 2; y p es 0, 1, 2, 3, o 4.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75338305P | 2005-12-23 | 2005-12-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058614A1 true AR058614A1 (es) | 2008-02-13 |
Family
ID=38218797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105721A AR058614A1 (es) | 2005-12-23 | 2006-12-21 | Compuesto de azaindol , composicion que lo comprende y su uso para preparar un medicamento |
Country Status (22)
| Country | Link |
|---|---|
| US (4) | US7282588B2 (es) |
| EP (1) | EP1962830B1 (es) |
| JP (1) | JP5140600B2 (es) |
| KR (1) | KR20080083680A (es) |
| CN (1) | CN101389324A (es) |
| AR (1) | AR058614A1 (es) |
| AU (1) | AU2006330587B2 (es) |
| BR (1) | BRPI0620341A2 (es) |
| CA (1) | CA2634787C (es) |
| CR (1) | CR10125A (es) |
| DK (1) | DK1962830T3 (es) |
| EA (1) | EA200870117A1 (es) |
| ES (1) | ES2408318T3 (es) |
| IL (1) | IL192351A0 (es) |
| MA (1) | MA30069B1 (es) |
| MX (1) | MX2008008320A (es) |
| NO (1) | NO20083267L (es) |
| PL (1) | PL1962830T3 (es) |
| PT (1) | PT1962830E (es) |
| SI (1) | SI1962830T1 (es) |
| TW (1) | TW200800990A (es) |
| WO (1) | WO2007076348A2 (es) |
Families Citing this family (89)
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|---|---|---|---|---|
| US20090298179A1 (en) * | 2003-04-29 | 2009-12-03 | Connie Erickson-Miller | Methods For Treating Degenerative Diseases/Injuries |
| EP1622609A4 (en) * | 2003-04-29 | 2008-09-03 | Smithkline Beecham Corp | METHODS OF TREATING DEGENERATIVE DISEASES / LESIONS |
| US20090048318A1 (en) * | 2003-04-29 | 2009-02-19 | Connie Erickson-Miller | Methods for treating degenerative diseases/injuries |
| US20090143453A1 (en) * | 2003-04-29 | 2009-06-04 | Connie Erickson-Miller | Methods for treating degenerative diseases/injuries |
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| SG10201506912RA (en) | 2005-12-13 | 2015-10-29 | Incyte Corp | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| PT1962830E (pt) * | 2005-12-23 | 2013-05-29 | Glaxosmithkline Llc | Inibidores azaindólicos de cinases aurora |
| EP1998777A1 (en) * | 2006-03-20 | 2008-12-10 | F. Hoffmann-La Roche AG | Methods of inhibiting btk and syk protein kinases |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| UY30892A1 (es) * | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| SI2740731T1 (sl) | 2007-06-13 | 2016-07-29 | Incyte Holdings Coroporation | Kristalinične soli inhibitorja za janus kinazo (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopen tilpropannitrila |
| AR070127A1 (es) * | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
| CA2722220C (en) | 2008-04-30 | 2016-06-07 | National Health Research Institutes | Fused bicyclic pyrimidine compounds as aurora kinase inhibitors |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| US9181182B2 (en) | 2008-10-17 | 2015-11-10 | Akaal Pharma Pty Ltd | S1P receptors modulators |
| JP2012505836A (ja) * | 2008-10-17 | 2012-03-08 | アカール ファーマ ピーティーワイ リミテッド | Ｓ１ｐ受容体モジュレーターおよびそれらの使用 |
| DE102008052943A1 (de) | 2008-10-23 | 2010-04-29 | Merck Patent Gmbh | Azaindolderivate |
| EP2198710A1 (de) | 2008-12-19 | 2010-06-23 | Bayer CropScience AG | Verwendung von 5-Pyridin-4yl-(1,3)Thiazole zur Bekämpfung phytopathogener Pilze |
| EP2376082B1 (en) * | 2008-12-22 | 2014-03-05 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-cd20 antibodies |
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