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
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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| CN108137586B (zh) | 2015-09-14 | 2021-04-13 | 辉瑞大药厂 | 作为LRRK2抑制剂的新颖咪唑并[4,5-c]喹啉和咪唑并[4,5-c][1,5]萘啶衍生物 |
| CR20180336A (es) | 2015-11-25 | 2018-08-06 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| KR20200129099A (ko) | 2018-01-30 | 2020-11-17 | 인사이트 코포레이션 | (1-(3-플루오로-2-(트리플루오로메틸)이소니코티닐)피페리딘-4-온)의 제조 방법 |
| CN112423759A (zh) | 2018-03-30 | 2021-02-26 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
| WO2020223456A1 (en) * | 2019-05-01 | 2020-11-05 | Nemucore Medical Innovations, Inc. | Degradation of aurora kinase (aurk) by conjugation of aurk inhibitors with e3 ligase ligand |
| CN114008046B (zh) * | 2019-06-27 | 2023-08-18 | 南京明德新药研发有限公司 | 作为cdk9抑制剂的氮杂吲哚连吡唑类化合物 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN112225723B (zh) * | 2020-12-16 | 2021-03-30 | 北京华氏开元医药科技有限公司 | 一种吲哚类衍生物、制备方法及应用 |
| WO2022135580A1 (zh) * | 2020-12-25 | 2022-06-30 | 南京明德新药研发有限公司 | 吡啶并吡咯类化合物的晶型、制备方法及其应用 |
| CN115572294B (zh) * | 2022-11-13 | 2023-11-21 | 药康众拓(江苏)医药科技有限公司 | 一种氘代氮杂吲哚联吡唑类化合物、药物组合物和用途 |
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|---|---|---|---|---|
| OA12514A (en) * | 1999-12-24 | 2006-05-29 | Aventis Pharma Ltd | Azaindoles. |
| GB9930698D0 (en) * | 1999-12-24 | 2000-02-16 | Rhone Poulenc Rorer Ltd | Chemical compounds |
| GB0102687D0 (en) * | 2001-02-02 | 2001-03-21 | Pharmacia & Upjohn Spa | Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them |
| CA2445568A1 (en) * | 2001-04-27 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Triazole-derived kinase inhibitors and uses thereof |
| WO2003000690A1 (en) | 2001-06-25 | 2003-01-03 | Aventis Pharmaceuticals Inc. | Synthesis of heterocyclic compounds employing microwave technology |
| JP4357295B2 (ja) * | 2001-08-03 | 2009-11-04 | バーテックス ファーマシューティカルズ インコーポレイテッド | ピラゾール誘導キナーゼインヒビターとその使用 |
| US6884889B2 (en) | 2002-03-25 | 2005-04-26 | Bristol-Myers Squibb Co. | Processes for the preparation of antiviral 7-azaindole derivatives |
| KR20050067383A (ko) * | 2002-08-06 | 2005-07-01 | 아스트라제네카 아베 | Ｔｉｅ2(ｔｅｋ) 활성을 갖는 축합 피리딘 및 피리미딘 |
| US7696225B2 (en) | 2003-01-06 | 2010-04-13 | Osi Pharmaceuticals, Inc. | (2-carboxamido)(3-Amino) thiophene compounds |
| AR045595A1 (es) * | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| EP2332940B1 (en) * | 2004-03-30 | 2012-10-31 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of JAK and other protein kinases |
| US7465726B2 (en) * | 2004-08-02 | 2008-12-16 | Osi Pharmaceuticals, Inc. | Substituted pyrrolo[2.3-B]pyridines |
| UA98449C2 (en) * | 2005-12-13 | 2012-05-25 | Инсайт Корпорейшин | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| EP1968568A4 (en) | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
| KR20080083680A (ko) * | 2005-12-23 | 2008-09-18 | 스미스클라인 비참 코포레이션 | 오로라 키나제의 아자인돌 억제제 |
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