AR045510A1 - Derivados de 1,3 diazoles - Google Patents

Derivados de 1,3 diazoles

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Publication number
AR045510A1
AR045510A1 ARP040103072A ARP040103072A AR045510A1 AR 045510 A1 AR045510 A1 AR 045510A1 AR P040103072 A ARP040103072 A AR P040103072A AR P040103072 A ARP040103072 A AR P040103072A AR 045510 A1 AR045510 A1 AR 045510A1
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Argentina
Prior art keywords
alkyl
substituted
ring
amino
optionally substituted
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ARP040103072A
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English (en)
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Novartis Ag
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Publication of AR045510A1 publication Critical patent/AR045510A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

La presente se refiere a derivados de 1,3 diazoles. Se describen compuestos y sus sales que son útiles para tratar condiciones que son mediadas por fosfatidilinositol 3-cinasa. También se describen composiciones farmacéuticas que contienen los compuestos y un procedimiento para la preparación de los compuestos. Reivindicación 1: Un compuesto de la fórmula (1) en forma libre o de sal, en donde: Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por piridilo; R3 es R6 y R4 es fluoro o haloalquilo C1-8, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por hidroxi o nitrilo, R3 es R6 y R4 es H o haloalquilo C1-8; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por nitrilo, R3 es fluoro y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por hidroxi, R3 es fluoro y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por di(alquilo C1-8)amino, R3 es R6, y R4 es haloalquilo C1-8, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por -O-C1-8alquilo-OH; R3 es R6 y R4 es fluoro o haloalquilo C1-8, o Ra es H o alquilo C1-4, Rb es -CH(CH3)-CH2-OH, R3 es R6, y R4 es fluoro, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por pirrolidinilo sustituido por alquilo C1-8, R3 es R6 y R4 es haloalquilo C1-8, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por oxazolilo sustituido por alquilo C1-8, R3 es R6 y R4 es nitrilo o imidazolilo, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por imidazolilo, R3 es R6 y R4 es fluoro; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por benzoimidazolilo, R3 es R6 y R4 es fluoro, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por isoxazolilo sustituido por alquilo C1-8, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por pirrolilo sustituido por alquilo C1-8, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por pirazolilo sustituido por alquilo C1-8, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por -CO-O-CH3-, -CO-O-butilo, -CO-di(alquil C1-8)amino, -CO-NH2, -NH-CO-C1-8-alquilo, -SO2-C1-8 alquilo, -CO-NH-Rc, en donde Rc es naftilo, o por -CO-NH-C1-8-alquilo opcionalmente sustituido por di(alquilo c1-8)-amino, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es -CH(CH3)-CO-NH-C1-8-alquilo o -CH(CH3)-CO-C1-8-alquilo, R3 es R6 y R4 es R7, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por -CH(OH)-CH2-OH; R3 es R6, y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por alcoxi C1-8, o por -S-alquilo C1-8, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por un anillo heterocíclico de 5 o 6 miembros teniendo uno o más átomos heterogéneos en el anillo seleccionados del grupo que consiste de O, N y S, ese anillo estando sustituido por oxo, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por un anillo heterocíclico de 5 o 6 miembros teniendo 3 o más átomos heterogéneos en el anillo seleccionados del grupo que consiste de O, N y S, ese anillo estando opcionalmente sustituido por alquilo C1-8, alquilo C1-8-di(alquilo C1-8)-amino, o por cicloalquilo C3-8, R3 es R6, y R4 es R7, o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por oxazolilo sustituido por alquilo C3-8, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es alquilo C1-8 sustituido por imidazolilo sustituido por alquilo c1-8 opcionalmente sustituido por hidroxi o alcoxi C1-8, R3 es R6, y R4 es R7; o Ra es h o alquilo C1-4, Rb es alquilo C1-8 sustituido por -CO-Het, en donde Het es un anillo heterocíclico de 5 o 6 miembros teniendo dos o más átomos heterogéneos en el anillo seleccionados del grupo que consiste de O, N y S, ese anillo estando opcionalmente sustituido por alquilo C1-8, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es un anillo heterocíclico de 5 o 6 miembros teniendo uno o más átomos heterogéneos en el anillo seleccionados del grupo que consiste de O, N, y S, ese anillo estando sustituido por oxo, R3 es R6 y R4 es R7; o Ra es H o alquilo C1-4, Rb es un anillo aza-bicíclico[3.2.1]oct-3-ilo opcionalmente sustituido por alquilo C1-8, R3 es R6 y R4 es R7; o Ra y Rb en conjunto forman un anillo de azetidina sustituido por alcoxicarbonilo C1-8, R3 es R6 y R4 es R7;o Ra y Rb juntos forman un anillo de pirrolidina sustituido por -CO-NH2 o nitrilo, R3 es R6 y R4 es R7, o Ra y Rb juntos forman un anillo de imidazo-piridina, R3 es R6 y R4 es R7; R2 es alquilo C1-4 o halógeno; R5 es H, halógeno o alquilo C1-8; R6 es halógeno, -SO2-CH3, -SO2-CF3, carboxi, -CO-NH2-, -CO-di(alquilo C1-8)amino, o un anillo heterocíclico de 5 o 6 miembros teniendo uno o más átomos heterogéneos en el anillo seleccionados del grupo que consiste de O, N y S, ese anillo estando opcionalmente sustituido por halógeno, ciano, oxo, hidroxi, carboxi, nitro, cicloalquilo C3-8, alquilcarbonilo C1-8, alcoxi C1-8 opcionalmente sustituido por aminocarbonilo, o alquilo C1-8 opcionalmente sustituido por hidroxi, alcoxi C1-8, alquilamino C1-8, o di(alquilo C1-8)amino; R7 es H, halógeno, -SO2-CH3, nitrilo, haloalquilo C1-8, imidazolilo, alquilo C1-8, -NR8R9-, o -SO2-NR8R9; y R8 y R9 son independientemente H, amino, alquilamino C1-8, di(alquilo c1-8)amino, o alquilo C1-8 opcionalmente sustituido por hidroxi, o R8 y R9 juntos forman un anillo heterocíclico de 5 a 10 miembros teniendo uno o más átomos heterogéneos en el anillo seleccionados del grupo que consiste de O, N y S, ese anillo estando opcionalmente sustituido por halógeno, ciano, oxo, hidroxi, carboxi, nitro, cicloalquilo C3-8, alquilcarbonilo C1-8, alcoxi C1-8 opcionalmente sustituido por aminocarbonilo, o alquilo C1-8 opcionalmente sustituido por hidroxi, alcoxi C1-8, alquilamino C1-8, o di(alquilo C1-8)amino.
ARP040103072A 2003-08-28 2004-08-26 Derivados de 1,3 diazoles AR045510A1 (es)

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GBGB0320197.7A GB0320197D0 (en) 2003-08-28 2003-08-28 Organic compounds

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AR045510A1 true AR045510A1 (es) 2005-11-02

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US (3) US7902375B2 (es)
EP (1) EP1689391B1 (es)
JP (1) JP4574618B2 (es)
KR (1) KR100774038B1 (es)
CN (1) CN1838953B (es)
AR (1) AR045510A1 (es)
AT (1) ATE429225T1 (es)
AU (1) AU2004268050B2 (es)
BR (1) BRPI0413934A (es)
CA (1) CA2533175A1 (es)
CY (1) CY1109227T1 (es)
DE (1) DE602004020793D1 (es)
DK (1) DK1689391T3 (es)
EC (1) ECSP066383A (es)
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GB (1) GB0320197D0 (es)
HK (1) HK1093688A1 (es)
HR (1) HRP20090340T1 (es)
IL (1) IL173035A0 (es)
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MA (1) MA28007A1 (es)
MX (1) MXPA06002217A (es)
MY (1) MY135050A (es)
NO (1) NO20061406L (es)
NZ (1) NZ545139A (es)
PE (1) PE20050872A1 (es)
PL (1) PL1689391T3 (es)
PT (1) PT1689391E (es)
RU (1) RU2382783C2 (es)
SI (1) SI1689391T1 (es)
TN (1) TNSN06064A1 (es)
TW (1) TWI347941B (es)
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Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
WO2005118543A1 (ja) * 2004-06-03 2005-12-15 Ono Pharmaceutical Co., Ltd. キナーゼ阻害薬およびその用途
WO2006037468A1 (en) * 2004-09-30 2006-04-13 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv reverse transcriptase inhibitors
AU2006251159B2 (en) 2005-05-24 2011-09-22 Merck Serono Sa Thiazole derivatives and use thereof
WO2006125803A1 (en) * 2005-05-24 2006-11-30 Laboratoires Serono S.A. Thiazole derivatives and use thereof
KR20080049767A (ko) 2005-08-26 2008-06-04 라보라뚜와르 세로노 에스. 에이. 피라진 유도체 및 ｐｉ３ｋ 억제제로서의 용도
GB0525671D0 (en) * 2005-12-16 2006-01-25 Novartis Ag Organic compounds
AU2007219509A1 (en) * 2006-01-18 2007-09-07 Siena Biotech S.P.A Modulators of alpha7 nicotinic acetylcholine receptors and therapeutic uses thereof
GB0608823D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of P13 kinase
GB0608854D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd P13 kinase inhibitors
GB0610243D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
GB0612630D0 (en) * 2006-06-26 2006-08-02 Novartis Ag Organic compounds
WO2008101979A1 (en) 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof
CN101820757A (zh) 2007-06-01 2010-09-01 普林斯顿大学托管委员会 通过调节宿主细胞代谢途径治疗病毒感染
JP2011506563A (ja) * 2007-12-20 2011-03-03 ノバルティス アーゲー ビスチアゾール誘導体、その製造方法および医薬品としてのその使用
AU2008340053A1 (en) 2007-12-20 2009-07-02 Novartis Ag Thiazole derivatives used as PI 3 kinase inhibitors
UA104147C2 (uk) 2008-09-10 2014-01-10 Новартис Аг Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань
CN101684106B (zh) * 2008-09-22 2013-06-12 北京摩力克科技有限公司 噻唑鎓盐类化合物及其治疗蛋白老化相关疾病的用途
KR20110115160A (ko) 2009-02-12 2011-10-20 메르크 세로노 에스. 에이. 2-모르폴리노-피리도〔3,2-ｄ〕피리미딘
PL2899191T3 (pl) * 2009-04-30 2018-01-31 Glaxo Group Ltd Indazole podstawione oksazolem jako inhibitory kinazy PI3
EP2440556A1 (en) * 2009-06-10 2012-04-18 Vertex Pharmaceuticals Incorporated Inhibitors of phosphatidylinositol 3-kinase
US8293753B2 (en) * 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
EP2448946B1 (en) 2009-07-02 2013-07-24 Novartis AG 2-carboxamide cycloamino ureas useful as pi3k inhibitors
JPWO2011048936A1 (ja) 2009-10-19 2013-03-07 大正製薬株式会社 アミノチアゾール誘導体
AU2010317883B2 (en) 2009-11-13 2015-08-06 Merck Serono S.A. Tricyclic pyrazol amine derivatives
WO2011097333A1 (en) 2010-02-03 2011-08-11 Signal Pharmaceuticals, Llc Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
GB201018124D0 (en) * 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
WO2013018733A1 (ja) * 2011-07-29 2013-02-07 富士フイルム株式会社 １，５－ナフチリジン誘導体又はその塩
US20130158023A1 (en) 2011-08-03 2013-06-20 Signal Pharmaceuticals, Llc Identification of gene expression as a predictive biomarker for lkb1 status
EP2763532B1 (en) 2011-10-05 2018-09-19 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
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
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
US9474757B2 (en) 2013-04-17 2016-10-25 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
AU2014254058B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a Dihydropyrazino-Pyrazine Compound and an androgen receptor antagonist for treating prostate cancer
UA119538C2 (uk) 2013-04-17 2019-07-10 Сігнал Фармасьютікалз, Елелсі Лікування злоякісної пухлини дигідропіразинопіразинами
TW201521725A (zh) 2013-04-17 2015-06-16 Signal Pharm Llc 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法
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
CN105392499B (zh) 2013-04-17 2018-07-24 西格诺药品有限公司 用于治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法
CN107474051B (zh) 2013-05-29 2020-10-30 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
WO2015160880A1 (en) 2014-04-16 2015-10-22 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
US10722513B2 (en) * 2015-03-23 2020-07-28 The University Of Melbourne Treatment of respiratory diseases
WO2017004383A1 (en) 2015-06-30 2017-01-05 Dana-Farber Cancer Institute, Inc. Inhibitors of egfr and methods of use thereof
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
JOP20190052A1 (ar) * 2016-09-22 2019-03-21 Astrazeneca Ab 5-[2-(بيريدين-2-يلامينو )-3،1 ثيازول-5-يال]-3،2 – ثنائي هيدرو- 1h- إيزوإندول 1--مشتق واحد واستخدامها كمثبطات مزدوجة للدلتا وغاما فوسفاتيديلينوسيتول 3-كيناز
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0519449A1 (en) * 1991-06-21 1992-12-23 Boehringer Mannheim Italia S.P.A. 2-Amino-4-aryl thiazoles with antiasthmatic and antiinflammatory activities on the respiratory tract
GB9823873D0 (en) * 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
WO2001017995A1 (en) 1999-09-10 2001-03-15 Merck & Co., Inc. Tyrosine kinase inhibitors
US6667300B2 (en) * 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
EP1294690A2 (en) 2000-06-21 2003-03-26 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
PL365170A1 (en) * 2000-07-26 2004-12-27 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl] carboxamide inhibitors of cyclin dependent kinases
WO2003015778A1 (en) * 2001-08-17 2003-02-27 Merck & Co., Inc. Tyrosine kinase inhibitors
TWI314928B (en) 2002-02-28 2009-09-21 Novartis A 5-phenylthiazole derivatives and use as pi3 kinase inhibitors

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