AR069798A1 - Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa. - Google Patents
Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa.Info
- Publication number
- AR069798A1 AR069798A1 ARP080105519A ARP080105519A AR069798A1 AR 069798 A1 AR069798 A1 AR 069798A1 AR P080105519 A ARP080105519 A AR P080105519A AR P080105519 A ARP080105519 A AR P080105519A AR 069798 A1 AR069798 A1 AR 069798A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compound
- halo
- obtainable
- radical
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (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)
- Epidemiology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Composiciones farmacéuticas y uso de los compuestos en el tratamiento de enfermedades mejoradas por la inhibicion de la fosfaditilinositol 3-cinasa. Reivindicacion 1: Un compuesto de la formula (1) en donde n representa 1 y m representa 1, 2, 3 o 4, o n representa 0 y m representa 0, 1, 2 o 3; R1 representa un radical arilo opcionalmente sustituido o heterociclilo opcionalmente sustituido; R2 representa un radical halo, ciano, nitro, hidroxi, fenilo, alquilo inferior, alcoxi inferior, alquilamino inferior, dialquilamino inferior, dialquilamino inferior-alquilo inferior, cicloalquilo, cicloalcoxi, en donde cada grupo alquilo o cicloalquilo puede estar monosustituido o polisustituido con radical halo, ciano, nitro, hidroxi, fenilo, y en donde cada fenilo puede estar monosustituido o polisustituido con radicales halo, ciano, nitro, hidroxi, alquilo inferior, dos sustituyentes R2 juntos forman un radical alcanodiilo o alquenodiilo, cada uno opcionalmente sustituido con radicales hidroxi o halo, para formar una porcion cíclica, o dos sustituyentes R2 juntos forman un enlace para formar un doble enlace; R3 representa un átomo de hidrogeno, un radical alquilo inferior, mono-, poli- o per-deuteroalquilo inferior, halo, haloalquilo inferior, hidroxialquilo inferior, dialquilamino inferior-alquilo inferior, o sales de los mismos. Reivindicacion 16: Un proceso para la manufactura de un compuesto de la formula 1, de conformidad con cualquiera de las reivindicaciones 1 a 7, que comprende hacer reaccionar un compuesto de la formula (2) en donde los sustituyentes son como los definidos en cualquiera de las reivindicaciones 1 a 5, ya sea con un compuesto de la formula (3) en donde los sustituyentes son como los definidos en cualquiera de las reivindicaciones 1 a 5 y R3 puede representar adicionalmente cloro, en presencia de un agente activador (ôMétodo Aö), o bien con un compuesto de la formula (4) en donde R1 es como el definido en cualquiera de las reivindicaciones 1 a 5; RG representa un grupo reactivo (tal como imidazolilcarbonilo) y es como el definido en cualquiera de las reivindicaciones 1 a 5, y puede representar adicionalmente cloro (ôMétodo Bö), en cada caso opcionalmente en presencia de un diluyente y opcionalmente en presencia de un auxiliar de reaccion, y opcionalmente recuperar el compuesto resultante de la formula (1), en forma libre o en forma de una sal, y opcionalmente transformar un compuesto de la formula (1), obtenible de conformidad con el Método A o el Método B, en un compuesto diferente de la formula (1), y/o transformar una sal obtenible de un compuesto de la formula (1), en una sal diferente del mismo y/o transformar un compuesto libre obtenible de la formula (1), en una sal del mismo, y/o separar un isomero obtenible de un compuesto de la formula (1), a partir de uno o más isomeros diferentes obtenibles de la formula (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07150228 | 2007-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069798A1 true AR069798A1 (es) | 2010-02-17 |
Family
ID=39273277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105519A AR069798A1 (es) | 2007-12-20 | 2008-12-18 | Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa. |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8940771B2 (es) |
| EP (1) | EP2240475B1 (es) |
| JP (1) | JP2011506560A (es) |
| KR (1) | KR20100093129A (es) |
| CN (1) | CN101952282A (es) |
| AR (1) | AR069798A1 (es) |
| AU (1) | AU2008340053A1 (es) |
| BR (1) | BRPI0820722A2 (es) |
| CA (1) | CA2710122A1 (es) |
| CL (1) | CL2008003822A1 (es) |
| CO (1) | CO6321276A2 (es) |
| CR (1) | CR11491A (es) |
| DO (1) | DOP2010000183A (es) |
| EA (1) | EA201000947A1 (es) |
| EC (1) | ECSP10010271A (es) |
| ES (1) | ES2437595T3 (es) |
| IL (1) | IL206286A0 (es) |
| MA (1) | MA31903B1 (es) |
| NI (1) | NI201000107A (es) |
| PA (1) | PA8809001A1 (es) |
| PE (1) | PE20091523A1 (es) |
| SM (1) | SMP201000096B (es) |
| SV (1) | SV2010003598A (es) |
| TN (1) | TN2010000293A1 (es) |
| TW (1) | TW200930364A (es) |
| UY (1) | UY31545A1 (es) |
| WO (1) | WO2009080694A1 (es) |
| ZA (1) | ZA201003928B (es) |
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| AR044519A1 (es) * | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
| UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| AU2010268058A1 (en) * | 2009-07-02 | 2012-01-19 | Novartis Ag | 2-carboxamide cycloamino ureas useful as PI3K inhibitors |
| US8293753B2 (en) * | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
| JP2013504543A (ja) | 2009-09-10 | 2013-02-07 | ノバルティス アーゲー | 二環ヘテロアリール類のエーテル誘導体 |
| CN102712648A (zh) | 2009-11-25 | 2012-10-03 | 诺瓦提斯公司 | 双环杂芳基的与苯稠合的6元含氧杂环衍生物 |
| JP2013528635A (ja) | 2010-06-17 | 2013-07-11 | ノバルティス アーゲー | ビフェニル置換１，３−ジヒドロ−ベンゾイミダゾール−２−イリデンアミン誘導体 |
| CN102947275A (zh) | 2010-06-17 | 2013-02-27 | 诺瓦提斯公司 | 哌啶基取代的1,3-二氢-苯并咪唑-2-亚基胺衍生物 |
| MX360157B (es) * | 2010-11-08 | 2018-10-24 | Novartis Ag | Uso de derivados de 2-carboxamida-cicloamino-urea en el tratamiento de enfermedades dependientes de egfr o de enfermedades que han adquirido resistencia a los agentes que tienen como objetivo los miembros de la familia egfr. |
| UA112539C2 (uk) | 2011-03-03 | 2016-09-26 | Новартіс Аг | Спосіб одержання похідних 2-карбоксамідциклоаміносечовини |
| JP2014507465A (ja) | 2011-03-08 | 2014-03-27 | ノバルティス アーゲー | フルオロフェニル二環式ヘテロアリール化合物 |
| WO2013052845A1 (en) * | 2011-10-05 | 2013-04-11 | The Board Of Trustees Of The Leland Stanford Junior University | Pi-kinase inhibitors with broad spectrum anti-infective activity |
| US9926309B2 (en) | 2011-10-05 | 2018-03-27 | The Board Of Trustees Of The Leland Stanford Junior University | Pi-kinase inhibitors with anti-infective activity |
| JP2015512416A (ja) * | 2012-03-30 | 2015-04-27 | ノバルティス アーゲー | 神経芽細胞腫、ユーイング肉腫または横紋筋肉腫の治療に使用するための化合物 |
| RU2014149145A (ru) | 2012-05-23 | 2016-07-20 | Ф. Хоффманн-Ля Рош Аг | Композиции и способы получения и применения эндодермальных клеток и гепатоцитов |
| DK2897644T3 (en) * | 2012-09-20 | 2018-09-10 | Novartis Ag | Pharmaceutical combination comprising a phosphatidylinositol 3-kinase inhibitor and an aromatase inhibitor |
| CN103232406B (zh) * | 2013-04-26 | 2015-07-29 | 北京大学 | 一种1,3-噻唑衍生物 |
| GB201308278D0 (en) * | 2013-05-08 | 2013-06-12 | Imp Innovations Ltd | Labelled Carboxylic Acids and Their Uses in Molecular Imaging |
| CA2987914C (en) * | 2015-06-30 | 2022-09-13 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| CN105294546B (zh) * | 2015-10-29 | 2017-12-08 | 天津市斯芬克司药物研发有限公司 | 一种吡啶化合物及其制备方法 |
| EP3419980A4 (en) | 2016-02-26 | 2019-07-03 | The Board of Trustees of the Leland Stanford Junior University | INHIBITORS OF PI-KINASE WITH ANTI-INFECTIOUS ACTIVITY |
| WO2019001307A1 (zh) * | 2017-06-26 | 2019-01-03 | 深圳市塔吉瑞生物医药有限公司 | 一种酰胺类化合物及包含该化合物的组合物及其用途 |
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-
2008
- 2008-12-18 PA PA20088809001A patent/PA8809001A1/es unknown
- 2008-12-18 EA EA201000947A patent/EA201000947A1/ru unknown
- 2008-12-18 AR ARP080105519A patent/AR069798A1/es unknown
- 2008-12-18 US US12/338,432 patent/US8940771B2/en active Active
- 2008-12-18 PE PE2008002131A patent/PE20091523A1/es not_active Application Discontinuation
- 2008-12-18 UY UY31545A patent/UY31545A1/es not_active Application Discontinuation
- 2008-12-18 JP JP2010538723A patent/JP2011506560A/ja not_active Ceased
- 2008-12-18 BR BRPI0820722-4A patent/BRPI0820722A2/pt not_active IP Right Cessation
- 2008-12-18 CN CN200880127267XA patent/CN101952282A/zh active Pending
- 2008-12-18 KR KR1020107015995A patent/KR20100093129A/ko not_active Application Discontinuation
- 2008-12-18 EP EP08865012.2A patent/EP2240475B1/en active Active
- 2008-12-18 ES ES08865012.2T patent/ES2437595T3/es active Active
- 2008-12-18 WO PCT/EP2008/067859 patent/WO2009080694A1/en active Application Filing
- 2008-12-18 AU AU2008340053A patent/AU2008340053A1/en not_active Abandoned
- 2008-12-18 CA CA2710122A patent/CA2710122A1/en not_active Abandoned
- 2008-12-19 TW TW097149899A patent/TW200930364A/zh unknown
- 2008-12-19 CL CL2008003822A patent/CL2008003822A1/es unknown
-
2010
- 2010-06-02 ZA ZA2010/03928A patent/ZA201003928B/en unknown
- 2010-06-08 MA MA32896A patent/MA31903B1/fr unknown
- 2010-06-10 IL IL206286A patent/IL206286A0/en unknown
- 2010-06-10 CR CR11491A patent/CR11491A/es not_active Application Discontinuation
- 2010-06-17 DO DO2010000183A patent/DOP2010000183A/es unknown
- 2010-06-18 EC EC2010010271A patent/ECSP10010271A/es unknown
- 2010-06-18 NI NI201000107A patent/NI201000107A/es unknown
- 2010-06-18 TN TN2010000293A patent/TN2010000293A1/fr unknown
- 2010-06-18 SV SV2010003598A patent/SV2010003598A/es not_active Application Discontinuation
- 2010-06-21 CO CO10074465A patent/CO6321276A2/es not_active Application Discontinuation
- 2010-07-20 SM SM201000096T patent/SMP201000096B/it unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PA8809001A1 (es) | 2009-07-23 |
| EP2240475A1 (en) | 2010-10-20 |
| ES2437595T3 (es) | 2014-01-13 |
| EP2240475B1 (en) | 2013-09-25 |
| MA31903B1 (fr) | 2010-12-01 |
| US8940771B2 (en) | 2015-01-27 |
| CL2008003822A1 (es) | 2009-06-26 |
| CO6321276A2 (es) | 2011-09-20 |
| US20090163469A1 (en) | 2009-06-25 |
| ECSP10010271A (es) | 2010-07-30 |
| IL206286A0 (en) | 2010-12-30 |
| CA2710122A1 (en) | 2009-07-02 |
| JP2011506560A (ja) | 2011-03-03 |
| SV2010003598A (es) | 2011-03-23 |
| KR20100093129A (ko) | 2010-08-24 |
| ZA201003928B (en) | 2011-04-28 |
| SMP201000096B (it) | 2011-09-09 |
| WO2009080694A1 (en) | 2009-07-02 |
| UY31545A1 (es) | 2009-08-03 |
| BRPI0820722A2 (pt) | 2015-06-16 |
| SMAP201000096A (it) | 2010-09-10 |
| PE20091523A1 (es) | 2009-10-29 |
| CR11491A (es) | 2010-08-05 |
| NI201000107A (es) | 2011-03-15 |
| TW200930364A (en) | 2009-07-16 |
| EA201000947A1 (ru) | 2011-02-28 |
| TN2010000293A1 (en) | 2011-11-11 |
| AU2008340053A1 (en) | 2009-07-02 |
| CN101952282A (zh) | 2011-01-19 |
| DOP2010000183A (es) | 2010-07-31 |
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