AR070079A1 - Derivados de morfolino pirimidina usados en enfermedades relacionadas con mtor quinasa y/o p13k - Google Patents
Derivados de morfolino pirimidina usados en enfermedades relacionadas con mtor quinasa y/o p13kInfo
- Publication number
- AR070079A1 AR070079A1 ARP080105784A ARP080105784A AR070079A1 AR 070079 A1 AR070079 A1 AR 070079A1 AR P080105784 A ARP080105784 A AR P080105784A AR P080105784 A ARP080105784 A AR P080105784A AR 070079 A1 AR070079 A1 AR 070079A1
- Authority
- AR
- Argentina
- Prior art keywords
- 6alkyl
- amino
- bis
- 6alkoxy
- aminoc1
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 101150097381 Mtor gene Proteins 0.000 title 1
- 102100023085 Serine/threonine-protein kinase mTOR Human genes 0.000 title 1
- ORXTYTVXABMVJS-UHFFFAOYSA-N morpholine;pyrimidine Chemical class C1COCCN1.C1=CN=CN=C1 ORXTYTVXABMVJS-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 45
- -1 carbocyclylC1-6alkyl Chemical group 0.000 abstract 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 12
- 125000005843 halogen group Chemical group 0.000 abstract 10
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 5
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 4
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000038030 PI3Ks Human genes 0.000 abstract 1
- 108091007960 PI3Ks Proteins 0.000 abstract 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 abstract 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- 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
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Una sal aceptable para uso farmacéutico del mismo, con los procesos para su preparacion, con composiciones farmacéuticas que los contienen y con su uso en terapias, por ejemplo en el tratamiento de enfermedades proliferativas tal como el cáncer y en particular de enfermedades mediadas por una mTOR quinasa y/o una o más enzimas PI3K. Reivindicacion 1: Un compuesto caracterizado porque es de la formula (1) o una sal aceptable para uso farmacéutico del mismo; en donde m es 0,1 , 2, 3 o 4; 1Y y Y2 son en forma independiente N o CR8 con la salvedad de que uno de 1Y y Y2 sea N y el otro sea CR8; X es un grupo de union seleccionado entre -CR4=CR5-, -CR4=CR5CR6R7-, -CR6R7CR5=CR4-, -C:::C-, -C:::CCR6R7-, -CR6R7C:::C-, -NR4CR6R7-, -OCR6R7-, -SCR6R7-, -S(O)CR6R7-, -S(O)2CR6R7-, -C(O)NR4CR6R7-, -NR4C(O)CR6R7-, -NR4C(O)NR5CR6R7-, -NR4S(O)2CR6R7-, -S(O)2NR4CR6R7-, -C(O)NR4-, -NR4C(O)-, -NR4C(O)NR5-, -S(O)2NR4- y - NR4S(O)2-; R1 es un grupo seleccionado entre hidrogeno, C1-6alquilo, C2-6aIquenilo, C2-6aIquinilo, carbociclilo, carbociclilC1-6alquilo, heterociclilo y heterociclilC1-6alquilo, donde dicho grupo está sustituido optativamente con uno o más grupos sustituyentes seleccionados entre halo, ciano, nitro, R9, -OR9, -SR9, -SOR9, -SO2R9, -COR9, -CO2R9, -CONR9R10, -NR9R10, -NR9COR10, -NR9CO2R10, -NR9CONR10R15, -NR9COCONR10R15 y -NR9SO2R10; R2 es un grupo seleccionado entre C1-6alquilo, carbociclilo y heterociclilo, donde dicho grupo está sustituido con -NR17CSNR18R19 y está sustituido optativamente con uno o más grupos sustituyentes seleccionados en forma independiente entre halo, ciano, nitro, -R11, -OR11, -SR11, -SOR11, -SO2R11, -COR11, -CO2R11, -CONR11R12, -NR11R12, -NR11COR12, y -NR11COCONR12R16 cada R3, cuando está presente, se selecciona en forma independiente entre halo, ciano, nitro, -R13, -OR13, -SR13, -SOR13, -SO2R13, -COR13, -CO2R13, -CONR13R14, -NR13R14, -NR13COR14, -NR13CO2R14 y -NR13SO2R14; R4 y R5 son en forma independiente hidrogeno o C1-6alquilo; o R1 y R4 junto con el átomo o los átomos a los cuales se encuentran unidos forman un anillo carbocíclico o heterocíclico de 4 a 10 miembros donde 1, 2 o 3 átomos de carbono del anillo se reemplazan optativamente con N, O o S y dicho anillo está sustituido optativamente con uno o más grupos sustituyentes seleccionados entre halo, ciano, nitro, hidroxi, oxo, C1-6alquilo, C1-6alcoxi, haIoC1-6alquilo, haloC1-6alcoxi, hidroxiC1-6alquilo, hidroxiC1-6alcoxi, C1-6alcoxiC1-6alquilo, C1-6alcoxiC1-6alcoxi, amino, C1-6alquilamino, bis(C1-6alquil)amino, aminoC1-6alquilo, (C1-6alquil)aminoC1-6alquilo, bis(C1-6alquil)aminoC1-6alquilo, cianoC1-6alquilo, C1-6alquilsulfonilo, C1-6alquilsulfonilamino, C1-6alquilsulfonil(C1-6alquil)amino, sulfamoílo, C1-6alquilsulfamoilo, bis(C1-6alquil)sulfamoílo, C1-6alcanoilamino, C1-6alcanoil(C1-6alquil)amino, carbamoilo, C1-6alquilcarbamoilo y bis(C1-6alquil)carbamoilo; R6 y R7 se seleccionan en forma independiente entre hidrogeno, halo, ciano, nitro y C1-6alquilo; R8 se selecciona entre hidrogeno, halo, ciano y C1-6alquilo; R9 y R10 son en forma independiente hidrogeno o un grupo seleccionado entre C1-6alquilo, carbociclilo, carbociclilC1-6alquilo, heterociclilo y heterociclilC1-6alquilo, donde dicho grupo está sustituido optativamente con uno o más grupos sustituyentes seleccionados entre halo, ciano, nitro, hidroxi, C1-6alquiIo, C1-6alcoxi, haloC1-6alquilo, haloC1-6alcoxi, hidroxiC1-6alquilo, hidroxiC1-6alcoxi, C1-6alcoxiC1-6alquilo, C1-6alcoxiC1-6aIcoxi, amino, C1-6alquilamino, bis(C1-6alquil)amino, aminoC1-6aIquilo, (C1-6alquil)aminoC1-6alquilo, bis(C1-6alquil)aminoC1-6alquilo, cianoC1-6aIquiIo, C1-6alquilsulfonilo, C1-6alquilsulfonilamino, C1-6alquiIsulfonil(C1-6aIquil)amino, sulfamoílo, C1-6alquilsulfamoilo, bis(C1-6alquil)sulfamoílo, C1-6aIcanoilamino, C1-6alcanoil(C1-6alquil)amino, carbamoilo, C1-6alquilcarbamoilo y bis(C1-6aquil)carbamoilo; R11, R12, R17 y R18 son en forma independiente hidrogeno o un grupo seleccionado entre C1-6alquilo, carbociclilo, carbociclilC1-6alquilo, heterociclilo y heterocicIilC1-6alquilo, donde dicho grupo está sustituido optativamente con uno o más grupos sustituyentes seleccionados entre halo, ciano, nitro, hidroxi, C1 6alquilo, C1-6alcoxi, haIoC1-6alquilo, haloC1-6alcoxi, hidroxiC1-6alquilo, hidroxiC1-6alcoxi, C1-6alcoxiC1-6alquilo, C1-6aIcoxiC1-6aIcoxi, amino, C1-6alquilamino, bis(C1-6alquil)amino, aminoC1-6alquilo, (C1-6alquiI)aminoC1-6alquilo, bis(C1-6alquil)aminoC1-6alquilo, cianoC1-6alquilo, C1-6aIquilsuIfoniIo, C1-6alcanoilamino, C1-6alcanoil(C1-6alquil)amino, carbamoilo, C1-6alquilcarbamoilo y bis(C1-6alquil)carbamoilo; R13, R14, R15, R16 y R19 son en forma independiente hidrogeno o un grupo seleccionado entre C1-6alquilo, carbociclilo, carbociclilC1-6alquilo, heterociclilo y heterocicIiIC1-6alquilo, donde dicho grupo está sustituido optativamente con uno o más grupos sustituyentes seleccionados entre halo, ciano, nitro, hidroxi, C1-6alquilo, C1-6aIcoxi, haloC1-6aIquilo, haloC1-6alcoxi, hidroxiC1-6alquilo, hidroxiC1-6alcoxi, C1-6alcoxiC1-6alquilo, C1-6alcoxiC1-6alcoxi, amino C1-6aIquilamino, bis(C1-6alquil)amino, aminoC1-6alquilo, (C1- 6alquil)aminoC1-6alquilo, bis(C1-6alquil)aminoC1-6alquilo, cianoC1-6aIquilo, C1-6alquilsulfonilo, C1-6alquilsulfonilamino, C1-6alquiIsulfonil(C1-6alquiI)amino, sulfamoílo, C1-6alquilsulfamoilo, bis(C1-6alquil)sulfamoílo, C1-6alcanoilamino, C1-6alcanoiI(C1-6alquil)amino, carbamoilo, C1-6alquilcarbamoilo y bis(C1-6alquil)carbamoilo; o R18 y R19 junto con el átomo de nitrogeno al cual se encuentran unidos forman un anillo heterocíclico de 3 a 10 miembros donde 1 o 2 átomos de carbono del anillo se reemplazan optativamente con N, O o S y dicho anillo está sustituido optativamente con uno o más grupos sustituyentes seleccionados entre halo, ciano, nitro, hidroxi, C1-6alquilo, C1-6alcoxi, haloC1-6alquilo, haloC1-6alcoxi, hidroxiC1-6aIquiIo, hidroxiC1-6alcoxi, C1-6alcoxiC1-6alquilo, C1-6alcoxiC1-6alcoxi, amino, C1-6alquilamino, bis(C1-6alquil)amino, aminoC1-6alquilo, (C1-6alquil)aminoC1-6alquilo, bis(C1-6alquil)aminoC1-6alquiIo, cianoC1-6alquilo, C1-6alquilsulfonilo, C1-6alquilsulfonilamino, C1-6alquilsultonil(C1-6alquil)amino, sulfamoilo, C1-6aIquilsulfamoilo, bis(C1-6alquiI)sulfamoilo, C1-6alcanoilamino, C1-6alcanoil(C1-6alquil)amino, carbamoilo, C1-6alquilcarbamoilo y bis(C1-6alquil)carbamoilo
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94853907P | 2007-07-09 | 2007-07-09 | |
| PCT/GB2008/050548 WO2009007750A1 (en) | 2007-07-09 | 2008-07-08 | Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070079A1 true AR070079A1 (es) | 2010-03-10 |
Family
ID=39791229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105784A AR070079A1 (es) | 2007-07-09 | 2008-12-30 | Derivados de morfolino pirimidina usados en enfermedades relacionadas con mtor quinasa y/o p13k |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8138183B2 (es) |
| EP (1) | EP2176238B1 (es) |
| JP (1) | JP5508260B2 (es) |
| KR (1) | KR20100042280A (es) |
| CN (1) | CN101809002B (es) |
| AR (1) | AR070079A1 (es) |
| AT (1) | ATE554075T1 (es) |
| AU (1) | AU2008273891B2 (es) |
| BR (1) | BRPI0814688A2 (es) |
| CA (1) | CA2692720A1 (es) |
| CL (1) | CL2008003940A1 (es) |
| CO (1) | CO6251364A2 (es) |
| CR (1) | CR11200A (es) |
| DO (1) | DOP2010000012A (es) |
| EA (1) | EA018708B1 (es) |
| EC (1) | ECSP109935A (es) |
| ES (1) | ES2385692T3 (es) |
| NI (1) | NI201000002A (es) |
| PE (1) | PE20100138A1 (es) |
| WO (1) | WO2009007750A1 (es) |
| ZA (1) | ZA200909224B (es) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008273889B2 (en) * | 2007-07-09 | 2012-03-08 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
| MX315904B (es) | 2008-05-30 | 2013-11-29 | Amgen Inc | Inhibidores de fosfoinosituro-3 cinasa. |
| US8785457B2 (en) | 2009-03-13 | 2014-07-22 | Cellzome Limited | Pyrimidine derivatives as mTOR inhibitors |
| UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| AR077628A1 (es) | 2009-07-02 | 2011-09-14 | Sanofi Aventis | Derivados de 6-(morfolin-4-il)-pirimidin-4(3h)-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fosforilacion de akt(pkb) |
| JP5680638B2 (ja) | 2009-07-02 | 2015-03-04 | サノフイ | 新規な(6−オキソ−1,6−ジヒドロピリミジン−2−イル)アミド誘導体、この調製およびakt(pkb)リン酸化インヒビターとしてのこの医薬的な使用 |
| MX2012005023A (es) | 2009-10-30 | 2012-06-19 | Ariad Pharma Inc | Metodos y composiciones para tratar cancer. |
| EP2992878A1 (en) | 2010-02-03 | 2016-03-09 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| ES2535116T3 (es) | 2010-03-04 | 2015-05-05 | Cellzome Limited | Derivados de urea sustituida con morfolino como inhibidores de mtor |
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| ES2612492T3 (es) | 2010-12-28 | 2017-05-17 | Sanofi | Nuevos derivados de piridiminas, su preparación y su utilización farmacéutica como inhibidores de fosforilación de AKT (PKB) |
| US20140163023A1 (en) | 2011-04-04 | 2014-06-12 | Cellzome Limited | Dihydropyrrolo pyrimidine derivatives as mtor inhibitors |
| MX373641B (es) | 2011-04-29 | 2020-05-04 | Selecta Biosciences Inc | Nanoportadores sintéticos tolerogénicos para la terapia contra alergias. |
| AU2012290056B2 (en) | 2011-08-03 | 2015-03-19 | Signal Pharmaceuticals, Llc | Identification of gene expression profile as a predictive biomarker for LKB1 status |
| RU2616619C2 (ru) | 2011-09-21 | 2017-04-18 | Селлзоум Лимитед | Морфолино-замещенные производные мочевины или карбамата в качестве ингибиторов mtor |
| WO2013049250A1 (en) | 2011-09-27 | 2013-04-04 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| BR112014008241A2 (pt) | 2011-10-07 | 2017-04-18 | Cellzome Ltd | composto, composição farmacêutica, métodos para tratar, controlar, retardar ou prevenir doenças e distúrbios, e para preparar um composto, e, uso de um composto |
| CA2871112C (en) | 2012-07-04 | 2020-05-12 | F. Hoffmann-La Roche Ag | Covalently linked antigen-antibody conjugates |
| FR2994572B1 (fr) * | 2012-08-17 | 2015-04-17 | Centre Nat Rech Scient | Pyrido[3,2-d]pyrimidines trisubstituees, leurs procedes de preparation et leurs utilisation en therapeutique |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| JP6417338B2 (ja) * | 2013-02-19 | 2018-11-07 | アムジエン・インコーポレーテツド | 癌の治療のためのmdm2阻害剤としてのシス−モルホリノン及び他の化合物 |
| EP2970237B1 (en) | 2013-03-14 | 2017-09-27 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| WO2014172432A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| JP6382945B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ,エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| KR102459285B1 (ko) | 2013-04-17 | 2022-10-27 | 시그날 파마소티칼 엘엘씨 | 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법 |
| TWI654979B (zh) | 2013-04-17 | 2019-04-01 | 美商標誌製藥公司 | 使用tor激酶抑制劑組合療法以治療癌症之方法 |
| KR102221029B1 (ko) | 2013-04-17 | 2021-02-26 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| WO2014172431A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| CN105283175A (zh) | 2013-05-03 | 2016-01-27 | 西莱克塔生物科技公司 | 用于降低的或增强的药效学作用的致耐受性合成纳米载体和治疗性大分子 |
| CN113831345A (zh) | 2013-05-29 | 2021-12-24 | 西格诺药品有限公司 | 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 |
| JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| EP3089996B1 (en) | 2014-01-03 | 2021-07-28 | F. Hoffmann-La Roche AG | Bispecific anti-hapten/anti-blood brain barrier receptor antibodies, complexes thereof and their use as blood brain barrier shuttles |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | Signal Pharmaceuticals, LLC | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| CA2947504A1 (en) * | 2014-06-26 | 2015-12-30 | F. Hoffmann-La Roche Ag | Anti-brdu antibodies and methods of use |
| WO2016020288A1 (en) | 2014-08-04 | 2016-02-11 | Nuevolution A/S | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| KR20170045344A (ko) | 2014-09-07 | 2017-04-26 | 셀렉타 바이오사이언시즈, 인크. | 항-바이러스 전달 벡터 면역 반응을 약화시키기 위한 방법 및 조성물 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| JP7523909B2 (ja) | 2017-03-11 | 2024-07-29 | セレクタ バイオサイエンシーズ インコーポレーテッド | 抗炎症剤および免疫抑制剤を含む合成ナノキャリアによる組み合わせ処置に関連する方法および組成物 |
| WO2018218197A2 (en) | 2017-05-26 | 2018-11-29 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| SG11201912403SA (en) | 2017-06-22 | 2020-01-30 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| LT3651768T (lt) | 2017-07-13 | 2024-04-25 | Board Of Regents, The University Of Texas System | Heterocikliniai atr kinazės inhibitoriai |
| EP3668839B1 (en) | 2017-08-17 | 2023-04-12 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
| WO2019178590A1 (en) | 2018-03-16 | 2019-09-19 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of atr kinase |
| JOP20220160A1 (ar) | 2019-12-20 | 2023-01-30 | Nuevolution As | مركبات فعّالة نحو مستقبلات نووية |
| EP4076657A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| MX2022012259A (es) | 2020-03-31 | 2022-12-08 | Nuevolution As | Compuestos activos frente a receptores nucleares. |
| MX2022012260A (es) | 2020-03-31 | 2022-11-30 | Nuevolution As | Compuestos activos frente a receptores nucleares. |
| CN111646985A (zh) * | 2020-06-01 | 2020-09-11 | 江苏集萃分子工程研究院有限公司 | 一种含嘧啶杂环抗肿瘤药物分子azd6738的合成方法 |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3922735A1 (de) | 1989-07-11 | 1991-01-24 | Hoechst Ag | Aminopyrimidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide |
| JP3649395B2 (ja) | 2000-04-27 | 2005-05-18 | 山之内製薬株式会社 | 縮合ヘテロアリール誘導体 |
| JP3810017B2 (ja) * | 2000-04-27 | 2006-08-16 | アステラス製薬株式会社 | 縮合ヘテロアリール誘導体 |
| AU2790502A (en) | 2000-11-10 | 2002-05-21 | Hoffmann La Roche | Pyrimidine derivatives and their use as neuropeptide y receptor ligands |
| MXPA05005477A (es) | 2002-11-21 | 2005-07-25 | Chiron Corp | Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer. |
| US20080058297A1 (en) | 2003-05-29 | 2008-03-06 | Synta Pharmaceuticals Corp. | Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss |
| GB0415364D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415367D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415365D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| US7772271B2 (en) * | 2004-07-14 | 2010-08-10 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| WO2007084413A2 (en) | 2004-07-14 | 2007-07-26 | Ptc Therapeutics, Inc. | Methods for treating hepatitis c |
| AU2005304393B2 (en) * | 2004-11-10 | 2012-09-27 | Synta Pharmaceuticals Corp. | IL-12 modulatory compounds |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| US7863270B2 (en) | 2005-05-13 | 2011-01-04 | Synta Pharmaceuticals Corp. | IL-12 modulatory compounds |
| EP1904504B1 (en) | 2005-05-20 | 2014-03-19 | MethylGene Inc. | Inhibitors of vegf receptor and hgf receptor signaling |
| DE102005024494A1 (de) | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Verwendung von Cyanopyrimidinen |
| PT1899329E (pt) | 2005-07-01 | 2012-01-13 | Irm Llc | Derivados de benzimidazole substituídos por pirimidina como inibidores de proteína quinase |
| CA2617042A1 (en) | 2005-07-29 | 2007-02-01 | Takeda Pharmaceutical Company Limited | Spiro-cyclic compound |
| CN101305010A (zh) * | 2005-09-01 | 2008-11-12 | 阿雷生物药品公司 | Raf抑制剂化合物及其用法 |
| JP2007091649A (ja) | 2005-09-29 | 2007-04-12 | Taisho Pharmaceut Co Ltd | ピリミジン誘導体及びその使用に関連する治療方法 |
| JP4531027B2 (ja) | 2005-09-29 | 2010-08-25 | 田辺三菱製薬株式会社 | 医薬組成物 |
| ES2535854T3 (es) | 2005-09-30 | 2015-05-18 | Miikana Therapeutics, Inc. | Compuestos de pirazol sustituidos |
| KR20080063809A (ko) | 2005-09-30 | 2008-07-07 | 버텍스 파마슈티칼스 인코포레이티드 | 야누스 키나아제의 억제제로서 유용한 데아자퓨린 |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| GB2431156A (en) | 2005-10-11 | 2007-04-18 | Piramed Ltd | 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase |
| TW200800963A (en) | 2005-10-28 | 2008-01-01 | Astrazeneca Ab | Chemical compounds |
| WO2007063868A1 (ja) | 2005-11-29 | 2007-06-07 | Toray Industries, Inc. | アリールメチレンウレア誘導体及びその用途 |
| GB0525080D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525081D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525083D0 (en) * | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| US20110034454A1 (en) | 2006-01-11 | 2011-02-10 | Allan Paul Dishington | Morpholino pyrimidine derivatives and their use in therapy |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EA200870217A1 (ru) | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| WO2007105023A1 (en) | 2006-03-15 | 2007-09-20 | Csir | Modulation of phosphoryl transferase activity of glutamine synthetase |
| JP5243696B2 (ja) | 2006-03-17 | 2013-07-24 | 田辺三菱製薬株式会社 | ベンゼン誘導体 |
| JPWO2007114323A1 (ja) | 2006-04-04 | 2009-08-20 | 大正製薬株式会社 | アミノピロリジン化合物 |
| KR20080110912A (ko) | 2006-04-19 | 2008-12-19 | 노파르티스 아게 | 인다졸 화합물 및 cdc7의 억제 방법 |
| WO2007126043A1 (ja) | 2006-04-27 | 2007-11-08 | Mitsubishi Tanabe Pharma Corporation | チアゾール環を含むカルボン酸誘導体の医薬用途 |
| GB0610909D0 (en) | 2006-06-05 | 2006-07-12 | Merck Sharp & Dohme | Therapeutic treatment |
| US8222256B2 (en) | 2006-07-05 | 2012-07-17 | Exelixis, Inc. | Methods of using IGFIR and ABL kinase modulators |
| WO2008023159A1 (en) | 2006-08-24 | 2008-02-28 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| EP2057129A1 (en) * | 2006-08-24 | 2009-05-13 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| US20080234262A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
| KR20100016431A (ko) | 2007-04-12 | 2010-02-12 | 에프. 호프만-라 로슈 아게 | 약학적 화합물 |
| AU2008273892A1 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
-
2008
- 2008-07-08 EP EP08776183A patent/EP2176238B1/en active Active
- 2008-07-08 KR KR1020107002942A patent/KR20100042280A/ko not_active Ceased
- 2008-07-08 US US12/668,056 patent/US8138183B2/en not_active Expired - Fee Related
- 2008-07-08 AU AU2008273891A patent/AU2008273891B2/en not_active Ceased
- 2008-07-08 ES ES08776183T patent/ES2385692T3/es active Active
- 2008-07-08 EA EA201000091A patent/EA018708B1/ru not_active IP Right Cessation
- 2008-07-08 CN CN2008801062258A patent/CN101809002B/zh not_active Expired - Fee Related
- 2008-07-08 CA CA 2692720 patent/CA2692720A1/en not_active Abandoned
- 2008-07-08 BR BRPI0814688A patent/BRPI0814688A2/pt not_active IP Right Cessation
- 2008-07-08 JP JP2010515602A patent/JP5508260B2/ja not_active Expired - Fee Related
- 2008-07-08 AT AT08776183T patent/ATE554075T1/de active
- 2008-07-08 WO PCT/GB2008/050548 patent/WO2009007750A1/en not_active Ceased
- 2008-12-19 PE PE2008002157A patent/PE20100138A1/es not_active Application Discontinuation
- 2008-12-30 CL CL2008003940A patent/CL2008003940A1/es unknown
- 2008-12-30 AR ARP080105784A patent/AR070079A1/es unknown
-
2009
- 2009-12-23 ZA ZA2009/09224A patent/ZA200909224B/en unknown
-
2010
- 2010-01-08 NI NI201000002A patent/NI201000002A/es unknown
- 2010-01-08 CR CR11200A patent/CR11200A/es not_active Application Discontinuation
- 2010-01-08 DO DO2010000012A patent/DOP2010000012A/es unknown
- 2010-02-03 EC EC2010009935A patent/ECSP109935A/es unknown
- 2010-02-09 CO CO10014081A patent/CO6251364A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EA018708B1 (ru) | 2013-10-30 |
| CN101809002B (zh) | 2013-03-27 |
| JP5508260B2 (ja) | 2014-05-28 |
| AU2008273891A1 (en) | 2009-01-15 |
| ZA200909224B (en) | 2011-05-25 |
| ECSP109935A (es) | 2010-03-31 |
| BRPI0814688A2 (pt) | 2017-06-06 |
| EP2176238B1 (en) | 2012-04-18 |
| CO6251364A2 (es) | 2011-02-21 |
| ES2385692T3 (es) | 2012-07-30 |
| CN101809002A (zh) | 2010-08-18 |
| NI201000002A (es) | 2010-10-12 |
| HK1142906A1 (en) | 2010-12-17 |
| AU2008273891B2 (en) | 2012-01-12 |
| CA2692720A1 (en) | 2009-01-15 |
| CR11200A (es) | 2010-06-17 |
| JP2010533160A (ja) | 2010-10-21 |
| ATE554075T1 (de) | 2012-05-15 |
| DOP2010000012A (es) | 2010-01-31 |
| CL2008003940A1 (es) | 2010-09-24 |
| US8138183B2 (en) | 2012-03-20 |
| EA201000091A1 (ru) | 2010-06-30 |
| PE20100138A1 (es) | 2010-03-20 |
| US20100249131A1 (en) | 2010-09-30 |
| EP2176238A1 (en) | 2010-04-21 |
| WO2009007750A1 (en) | 2009-01-15 |
| KR20100042280A (ko) | 2010-04-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR070079A1 (es) | Derivados de morfolino pirimidina usados en enfermedades relacionadas con mtor quinasa y/o p13k | |
| AR062526A1 (es) | DERIVADOS DE 4-(3-METILMORFOLIN-4-IL)PIRIMIDINA Y MORFOLIN-4-IL-PIRIMIDINA COMO INHIBIDORES DE MTOR QUINASA Y PI3K, UNA COMPOSICIoN FARMACEUTICA QUE LOS COMPRENDE Y EL USO DE LOS MISMOS EN LA FABRICACION DE MEDICAMENTOS PARA EL TRATAMIENTO DE DIVERSOS TIPOS DE CANCER. | |
| AR067478A1 (es) | Compuestos derivados de morfolina pirimidina | |
| CO6251271A2 (es) | Derivados de pirimidina trisustituida para el tratamiento de enfermedades proliferativas | |
| CO6351793A2 (es) | \"derivados de indol macrociclicos utiles como inhibidores del virus de la hepatitis | |
| CO6210729A2 (es) | Derivados de sulfonil-fenil-2h-[1,2,4]oxadiazol-5-ona procedimientos para su preparacion y su uso como agente farmaceutico | |
| UY29177A1 (es) | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos | |
| CO6321276A2 (es) | Derivados de tiazol usados como inhibidores de pi3- cinasa | |
| AR060768A1 (es) | Compuestos de imidazol sustituidos inhibidores del factor x, composiciones farmaceuticas que los contienen y usos como agentes antitromboticos. | |
| PE20181298A1 (es) | Inhibidores de bromodominio bivalentes y usos de los mismos | |
| GT200600518A (es) | Derivados de pirimidina | |
| PE20141352A1 (es) | Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento | |
| AR059957A1 (es) | DERIVADOS DE ESPIROINDOLINONA, MÉTODOS PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACÉUTICA QUE LOS CONTIENE Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DEL CÁNCER. | |
| AR066659A1 (es) | Derivados de espiroindolinona | |
| UY31183A1 (es) | Derivados de pirazinona y procesos para su preparación | |
| AR070479A1 (es) | Derivado heterociclico fusionado y su uso | |
| AR063602A1 (es) | Derivados de espiroindolinona, formulaciones farmaceuticas que los contienen y su uso en la obtencion de un medicamento para el tratamiento de trastornos oncologicos. | |
| AR061548A1 (es) | 3-aminopirrolidino-4-lactamas sustituidas como inhibidoras de dipeptidilpeptidasa iv (dpp-iv), composiciones farmaceuticas que las comprenden y el uso de las mismas en el tratamiento de la diabetes ii. | |
| UY31906A (es) | Derivados de n-cicloalquil-3-fenilnicotinamida que inhiben pgds, sus composiciones, su uso para el tratamiento por ejemplo de afecciones alérgicas y respiratorias. | |
| AR080865A1 (es) | Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer. | |
| CU20090132A7 (es) | Compuestos tricíclicos, composiciones y procedimientos | |
| UY29316A1 (es) | Miméticos de glucocorticoides, métodos para prepararlos, composiciones farmacéuticas, y usos de los mismos. | |
| AR078278A1 (es) | Antagonistas de la tiazol y oxazol hepcidina, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de anemias y enfermedades asociadas a deficiencias de hierro. | |
| AR063643A1 (es) | Compuestos quimicos derivados de quinolina, un metodo de preparacion y composiciones farmaceuticas | |
| MX2017004541A (es) | Derivados espirodiamina como inhibidores de la aldosterona sintasa. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |