ECSP056127A - Inhibidores de 3-quinasa de fosfatidil-inositol - Google Patents

Inhibidores de 3-quinasa de fosfatidil-inositol

Info

Publication number
ECSP056127A
ECSP056127A EC2005006127A ECSP056127A ECSP056127A EC SP056127 A ECSP056127 A EC SP056127A EC 2005006127 A EC2005006127 A EC 2005006127A EC SP056127 A ECSP056127 A EC SP056127A EC SP056127 A ECSP056127 A EC SP056127A
Authority
EC
Ecuador
Prior art keywords
inositol
fosfatidil
kinase inhibitors
compounds
kinase
Prior art date
Application number
EC2005006127A
Other languages
English (en)
Inventor
Ian Bruce
Nicola Elaine Press
Judy Hayler
Bernard Cuenoud
Thomas Hugo Keller
Gaynor Elizabeth Pilgrim
Grand Darren Mark Le
Cathy Ritchie
Barbara Valade
Emma Budd
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of ECSP056127A publication Critical patent/ECSP056127A/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

Abstract

Los compuestos de la Fórmula (I) en forma libre o de sal, en donde R1, R2, R3, y R4 tienen los significados indicados en la memoria descriptiva, son útiles para el tratamiento de condiciones que sean mediadas por la 3-quinasa de fosfatidil-inositol. También se describen composiciones farmacéuticas que contienen a los compuestos, y un proceso para preparar los compuestos.
EC2005006127A 2003-05-02 2005-10-28 Inhibidores de 3-quinasa de fosfatidil-inositol ECSP056127A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB0310234 2003-05-02

Publications (1)

Publication Number Publication Date
ECSP056127A true ECSP056127A (es) 2006-03-01

Family

ID=33397059

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005006127A ECSP056127A (es) 2003-05-02 2005-10-28 Inhibidores de 3-quinasa de fosfatidil-inositol

Country Status (28)

Country Link
US (3) US20070032487A1 (es)
EP (2) EP1622897B1 (es)
JP (1) JP4510807B2 (es)
KR (1) KR100725885B1 (es)
CN (2) CN1816549B (es)
AR (1) AR044519A1 (es)
AT (1) ATE445614T1 (es)
AU (2) AU2004234068B2 (es)
BR (1) BRPI0410037B8 (es)
CA (1) CA2524401C (es)
CL (1) CL2004000917A1 (es)
DE (1) DE602004023602D1 (es)
EC (1) ECSP056127A (es)
ES (2) ES2546851T3 (es)
HK (1) HK1091810A1 (es)
IL (1) IL171536A (es)
IS (1) IS8152A (es)
MA (1) MA27774A1 (es)
MX (1) MXPA05011740A (es)
NO (1) NO20055714L (es)
PE (1) PE20050147A1 (es)
PL (1) PL1622897T3 (es)
PT (1) PT1622897E (es)
RU (2) RU2481346C2 (es)
TN (1) TNSN05278A1 (es)
TW (1) TW200519106A (es)
WO (1) WO2004096797A1 (es)
ZA (1) ZA200508603B (es)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
TW200533357A (en) * 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
SE0402735D0 (sv) * 2004-11-09 2004-11-09 Astrazeneca Ab Novel compounds
CN101115749B (zh) * 2004-12-17 2011-06-22 安姆根有限公司 氨基嘧啶化合物和使用方法
US20060178388A1 (en) * 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
BRPI0610341A2 (pt) * 2005-05-24 2010-06-15 Serono Lab derivados de tiazol e uso dos mesmos
BRPI0611029A2 (pt) * 2005-05-24 2010-08-10 Serono Lab derivados de tiazol e uso dos mesmos
US20090233896A1 (en) * 2005-06-09 2009-09-17 Arrington Kenneth L Inhibitors of checkpoint kinases
GB2431156A (en) * 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
WO2007098826A2 (en) * 2006-01-18 2007-09-07 Siena Biotech S.P.A. Modulators of alpha7 nicotinic acetylcholine receptors and therapeutic uses thereof
CA2636077C (en) * 2006-01-18 2012-01-03 Amgen Inc. Thiazole compounds as protein kinase b (pkb) inhibitors
JP2009523769A (ja) * 2006-01-23 2009-06-25 ラボラトワール セローノ ソシエテ アノニム チアゾール誘導体及びこれらの使用
CA2682189C (en) * 2006-04-07 2015-12-08 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
CN101484452A (zh) * 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 噻唑衍生物及其作为抗肿瘤药物的用途
GB0612630D0 (en) 2006-06-26 2006-08-02 Novartis Ag Organic compounds
JP2010502628A (ja) * 2006-09-01 2010-01-28 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 ホスファチジルイノシトール3−キナーゼの阻害剤として有用な5−(2−フリル)−1,3−チアゾール誘導体
GB0620059D0 (en) * 2006-10-10 2006-11-22 Ucb Sa Therapeutic agents
GB0620818D0 (en) 2006-10-19 2006-11-29 Ucb Sa Therapeutic agents
JP2010519309A (ja) * 2007-02-20 2010-06-03 ノバルティス アーゲー 脂質キナーゼおよびmTORのデュアル阻害剤としてのイミダゾキノリン
TW200906825A (en) * 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
EP2581081A3 (en) 2007-06-01 2013-07-31 The Trustees Of Princeton University Treatment of viral infections by modulation of host cell metabolic pathways
WO2009011871A2 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
CA2692713A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
US20100298286A1 (en) * 2007-12-20 2010-11-25 Novartis Ag Organic Compounds
JP2011506560A (ja) * 2007-12-20 2011-03-03 ノバルティス アーゲー Pi3キナーゼ阻害剤として用いられるチアゾール誘導体
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
EP2253618A1 (en) 2008-02-27 2010-11-24 Takeda Pharmaceutical Company Limited Compound having 6-membered aromatic ring
UA104147C2 (uk) 2008-09-10 2014-01-10 Новартис Аг Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань
CN102395585A (zh) * 2009-01-30 2012-03-28 米伦纽姆医药公司 杂芳基化合物和其作为pi3k抑制剂的用途
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201103943A (en) * 2009-04-27 2011-02-01 Shionogi & Co Urea derivative having pi3k inhibitory activity
DK2899191T3 (da) * 2009-04-30 2017-11-13 Glaxo Group Ltd Oxazol-substituerede indazoler som pi3-kinaseinhibitorer
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
MX2012000178A (es) 2009-07-02 2012-02-28 Novartis Ag 2-carboxamida-cicloamino-ureas utiles como inhibidores de pi3k.
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
CA2788678C (en) 2010-02-03 2019-02-26 Signal Pharmaceuticals, Llc Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
PE20131304A1 (es) 2010-08-11 2013-11-14 Millennium Pharm Inc Heteroarilos y sus usos
JP2013533318A (ja) 2010-08-11 2013-08-22 ミレニアム ファーマシューティカルズ, インコーポレイテッド ヘテロアリールおよびその使用
UY33671A (es) 2010-10-13 2012-04-30 Millenium Pharmaceuticals Inc Heteroarilos y sus usos
WO2012062694A1 (en) * 2010-11-08 2012-05-18 Novartis Ag Use of 2-carboxamide cycloamino urea derivatives in the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members
AU2015203865B2 (en) * 2010-11-08 2016-11-03 Novartis Ag Use of 2-carboxamide cycloamino urea derivatives in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members
UA112539C2 (uk) 2011-03-03 2016-09-26 Новартіс Аг Спосіб одержання похідних 2-карбоксамідциклоаміносечовини
NZ615593A (en) * 2011-04-25 2015-05-29 Novartis Ag Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor
UA114178C2 (uk) 2011-07-01 2017-05-10 Новартіс Аг Комбінація, що включає інгібітор cdk4/6 і інгібітор pi3k, для лікування раку
EP2739751A1 (en) 2011-08-03 2014-06-11 Signal Pharmaceuticals, LLC Identification of gene expression profile as a predictive biomarker for lkb1 status
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
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
EP3251673A1 (en) 2012-12-13 2017-12-06 IP Gesellschaft für Management mbH Combination therapy comprising a cdk4/6 inhibitor and a pi3k inhibitor for use in the treatment of cancer
TWI628170B (zh) 2013-02-05 2018-07-01 先正達合夥公司 植物生長調節化合物
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
CA2909625C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
MX2015014590A (es) 2013-04-17 2016-03-03 Signal Pharm Llc Tratamiento de cancer con dihidropirazino-pirazinas.
EA030726B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ, СПОСОБЫ, ТВЕРДЫЕ ФОРМЫ И СПОСОБЫ ПРИМЕНЕНИЯ, ОТНОСЯЩИЕСЯ К 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1H-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1H)-ОНУ
EA030808B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ПРИМЕНЕНИЕ 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1Н-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1Н)-ОНА В ЛЕЧЕНИИ МУЛЬТИФОРМНОЙ ГЛИОБЛАСТОМЫ
CN105339008A (zh) 2013-04-17 2016-02-17 西格诺药品有限公司 用于治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯酰胺的组合疗法
US9937169B2 (en) 2013-04-17 2018-04-10 Signal Pharmaceuticals, Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
MX2015015880A (es) 2013-05-29 2016-05-31 Signal Pharm Llc Composiciones farmaceuticas de 7-(6-(2-hidroxipropan-2-il)piridin- 3-il)-1-((trans)-4-metoxiciclohexil)-3,4-dihidropirazino[2,3-b]pi razin-2(1h)-ona, una forma solida del mismo y metodos de su uso.
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
CN104803921A (zh) * 2015-03-14 2015-07-29 长沙深橙生物科技有限公司 一种苯取代嘧啶衍生物的制备方法
CN104744376A (zh) * 2015-03-14 2015-07-01 长沙深橙生物科技有限公司 一种2-异丙基嘧啶衍生物的制备方法
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
CN110996955A (zh) 2017-06-22 2020-04-10 细胞基因公司 以乙型肝炎病毒感染为特征的肝细胞癌的治疗
WO2019136514A1 (en) * 2018-01-15 2019-07-18 University Of South Australia 5-(pyrimidin-4-yl)thiazol-2-yl urea derivatives as therapeutic agents
CN112752761B (zh) 2018-08-21 2024-03-29 杏林制药株式会社 双环杂芳族环衍生物
WO2021142006A1 (en) * 2020-01-07 2021-07-15 Disarm Therapeutics, Inc. Inhibitors of sarm1

Family Cites Families (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
GB8302591D0 (en) * 1983-01-31 1983-03-02 Fujisawa Pharmaceutical Co Thiazole derivatives
US4649146A (en) 1983-01-31 1987-03-10 Fujisawa Pharmaceutical Co., Ltd. Thiazole derivatives and pharmaceutical composition comprising the same
DE3703435A1 (de) * 1987-02-05 1988-08-18 Thomae Gmbh Dr K Neue thiazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US5229402A (en) 1988-04-15 1993-07-20 Taiho Pharmaceutical Company, Ltd. Carbamoyl-2-pyrrolidinone compounds
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
CA2038379C (en) 1990-03-22 2002-11-05 Norma G. Delaney Trifluoromethyl mercaptan and mercaptoacyl derivatives and method of using same
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
EP0946587A2 (en) 1996-12-16 1999-10-06 Fujisawa Pharmaceutical Co., Ltd. New amide compounds
US6187797B1 (en) 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
TW528755B (en) 1996-12-24 2003-04-21 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
US6436966B1 (en) 1997-10-27 2002-08-20 Takeda Chemical Ind., Ltd. Adenosine A3 receptor antagonists
GB9723589D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723590D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
PE20000270A1 (es) 1998-02-14 2000-05-20 Glaxo Group Ltd Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
JP2002518380A (ja) 1998-06-18 2002-06-25 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存キナーゼの炭素置換アミノチアゾール抑制剤
US6495528B1 (en) 1998-06-23 2002-12-17 Smithkline Beecham Corporation 2-(Purin -9-yl)-tetrahydrofuran-3,4-diol derivatives
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
JP4369053B2 (ja) 1998-06-30 2009-11-18 ダウ グローバル テクノロジーズ インコーポレイティド ポリマーポリオール及びその製造方法
CA2347512C (en) 1998-10-16 2005-12-06 Pfizer Inc. Adenine derivatives
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
US7101899B1 (en) * 1999-04-23 2006-09-05 Takeda Pharmaceutical Company Limited 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
PL203116B1 (pl) 1999-05-04 2009-08-31 Schering Corp Piperazynopiperydynowa pochodna użyteczna jako antagonista CCR5, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie
CN1524527A (zh) 1999-05-04 2004-09-01 ���鹫˾ 用作ccr5拮抗剂的哌啶衍生物
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB9913932D0 (en) 1999-06-15 1999-08-18 Pfizer Ltd Purine derivatives
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
ATE309241T1 (de) * 1999-09-10 2005-11-15 Merck & Co Inc Tyrosin kinase inhibitoren
CO5180581A1 (es) 1999-09-30 2002-07-30 Pfizer Prod Inc Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
CN100355751C (zh) 2000-03-29 2007-12-19 西克拉塞尔有限公司 2-取代的4-杂芳基-嘧啶、其组合物及其用途
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
KR100751981B1 (ko) 2000-06-27 2007-08-28 라보라토리오스 살바트, 에스.에이. 아릴알킬아민으로부터 유도된 카바메이트
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
EP1305329B2 (en) 2000-08-05 2015-03-18 Glaxo Group Limited 6.alpha.,9.alpha.-difluoro-17.alpha.-(2-furanylcarboxyl)oxy-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
EP1415987B1 (en) 2000-10-20 2007-02-28 Eisai R&D Management Co., Ltd. Nitrogenous aromatic ring compounds as anti cancer agents
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
CA2441896A1 (en) 2000-12-22 2002-07-04 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as m3 antagonists
CN1250545C (zh) 2000-12-28 2006-04-12 阿尔米雷尔普罗迪斯制药有限公司 新的奎宁环衍生物类及含有这类衍生物的药物组合物
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
BR0209271A (pt) 2001-04-30 2004-06-15 Glaxo Group Ltd Composto, uso de um composto composição farmacêutica, formulação em aerossol farmacêutica, método para o tratamento de um paciente humano ou animal com uma condição inflamatória e/ou alérgica, e, processo para a preparação de um composto
EP1256578B1 (en) 2001-05-11 2006-01-11 Pfizer Products Inc. Thiazole derivatives and their use as cdk inhibitors
US20040171576A1 (en) 2001-05-25 2004-09-02 Michael Yeadon Adenosine a2a receptor agonist and an anticholinergic agent in combination for treating obstructive airways diseases
US20040248867A1 (en) 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
EP1578910A4 (en) 2001-06-21 2008-06-04 Verenium Corp NITRILASES
CN100496493C (zh) * 2001-08-13 2009-06-10 詹森药业有限公司 2-氨基-4,5-三取代噻唑基衍生物
US7265134B2 (en) 2001-08-17 2007-09-04 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1760082A1 (en) 2001-09-28 2007-03-07 Cyclacel Limited N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-N-phenylamines as anti-proliferative compounds
CZ2004501A3 (cs) 2001-10-17 2004-09-15 Ucb, S.A. Chinuklidinové deriváty, způsoby jejich přípravy a jejich použití jako M2 a/nebo M3 inhibitoru muskarinového receptoru
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
IL162596A0 (en) 2001-12-20 2005-11-20 S A L V A T Lab Sa 1-Alkyl-1-azoniabicyclo Ä2.2.2Ü octane carbamate derivatives and their use as muscarinic receptor ntagonists
AU2003202044A1 (en) 2002-01-15 2003-09-09 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
AU2003201693A1 (en) 2002-01-21 2003-09-02 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
PE20030968A1 (es) 2002-02-28 2004-01-12 Novartis Ag Derivados de 5-feniltiazol como inhibidores de cinasas
ES2298508T3 (es) 2002-03-26 2008-05-16 Boehringer Ingelheim Pharmaceuticals Inc. Mimeticos de glucocorticoides, metodos para prepararlos, composiciones farmaceuticas y sus usos.
CA2477764A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2003086408A1 (en) 2002-04-10 2003-10-23 University Of Virginia Patent Foundation Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
EP1517895B1 (en) 2002-06-25 2007-03-14 Merck Frosst Canada Ltd. 8-(biaryl) quinoline pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
EP1519922A1 (en) 2002-07-02 2005-04-06 Merck Frosst Canada & Co. Di-aryl-substituted ethane pyridone pde4 inhibitors
PT1521733E (pt) 2002-07-08 2014-10-29 Pfizer Prod Inc Moduladores do recetor de glucocorticoides
AR040962A1 (es) 2002-08-09 2005-04-27 Novartis Ag Compuestos derivados de tiazol 1,3-2-ona, composicion farmaceutica y proceso de preparacion del compuesto
AU2003288956A1 (en) 2002-10-30 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
EP1567487A4 (en) 2002-11-15 2005-11-16 Bristol Myers Squibb Co OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
JP2007504255A (ja) 2003-09-06 2007-03-01 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 Atp結合カセットトランスポーターの調節因子
ZA200605624B (en) 2004-01-12 2007-11-28 Applied Research Systems Thiazole derivatives and use thereof
SE0402735D0 (sv) 2004-11-09 2004-11-09 Astrazeneca Ab Novel compounds
BRPI0610341A2 (pt) 2005-05-24 2010-06-15 Serono Lab derivados de tiazol e uso dos mesmos
BRPI0611029A2 (pt) 2005-05-24 2010-08-10 Serono Lab derivados de tiazol e uso dos mesmos
US7655446B2 (en) 2005-06-28 2010-02-02 Vertex Pharmaceuticals Incorporated Crystal structure of Rho-kinase I kinase domain complexes and binding pockets thereof
DE102005048072A1 (de) 2005-09-24 2007-04-05 Bayer Cropscience Ag Thiazole als Fungizide
ZA200805227B (en) 2005-12-12 2009-11-25 Genelabs Tech Inc N-(5-memebered heteroarmatic ring)-amido anti-viral compounds
GB0525671D0 (en) 2005-12-16 2006-01-25 Novartis Ag Organic compounds
JP2009523769A (ja) 2006-01-23 2009-06-25 ラボラトワール セローノ ソシエテ アノニム チアゾール誘導体及びこれらの使用
GB0610243D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
TW200827368A (en) 2006-11-21 2008-07-01 Genelabs Tech Inc Amido anti-viral compounds
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
CN101687790B (zh) 2007-05-25 2015-02-11 Abbvie公司 作为代谢型谷氨酸受体2(mglu2受体)的正向调节剂的杂环化合物
WO2009003009A1 (en) 2007-06-26 2008-12-31 Enanta Pharmaceuticals, Inc. Substituted pyrrolidine as anti-infectives
AU2008275891B2 (en) 2007-07-19 2013-10-10 H.Lundbeck A/S 5-membered heterocyclic amides and related compounds
JP2011506560A (ja) 2007-12-20 2011-03-03 ノバルティス アーゲー Pi3キナーゼ阻害剤として用いられるチアゾール誘導体
US20100298286A1 (en) 2007-12-20 2010-11-25 Novartis Ag Organic Compounds
UA104147C2 (uk) * 2008-09-10 2014-01-10 Новартис Аг Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas

Also Published As

Publication number Publication date
EP2157091B1 (en) 2015-06-10
CN1816549B (zh) 2010-09-29
RU2009134044A (ru) 2011-03-20
NO20055714L (no) 2006-02-02
MA27774A1 (fr) 2006-02-01
EP1622897A1 (en) 2006-02-08
DE602004023602D1 (en) 2009-11-26
BRPI0410037B8 (pt) 2021-05-25
AU2008255157A1 (en) 2009-01-08
CN1816549A (zh) 2006-08-09
US20070032487A1 (en) 2007-02-08
TW200519106A (en) 2005-06-16
AU2008255157B2 (en) 2011-02-03
ATE445614T1 (de) 2009-10-15
CA2524401C (en) 2011-11-22
KR100725885B1 (ko) 2007-06-08
US20130172349A1 (en) 2013-07-04
ES2331883T3 (es) 2010-01-19
TNSN05278A1 (en) 2007-07-10
ES2546851T3 (es) 2015-09-29
HK1091810A1 (en) 2007-01-26
EP1622897B1 (en) 2009-10-14
AU2004234068A1 (en) 2004-11-11
CA2524401A1 (en) 2004-11-11
RU2384580C2 (ru) 2010-03-20
RU2005137358A (ru) 2006-07-27
IS8152A (is) 2005-11-25
CL2004000917A1 (es) 2005-02-11
JP2006525266A (ja) 2006-11-09
NO20055714D0 (no) 2005-12-02
US8404684B2 (en) 2013-03-26
JP4510807B2 (ja) 2010-07-28
EP2157091A1 (en) 2010-02-24
AR044519A1 (es) 2005-09-14
ZA200508603B (en) 2006-12-27
BRPI0410037B1 (pt) 2018-01-16
MXPA05011740A (es) 2006-01-26
CN101648949A (zh) 2010-02-17
BRPI0410037A (pt) 2006-04-25
PE20050147A1 (es) 2005-05-05
US20110105535A1 (en) 2011-05-05
AU2004234068B2 (en) 2008-09-11
PT1622897E (pt) 2009-12-10
RU2481346C2 (ru) 2013-05-10
PL1622897T3 (pl) 2010-03-31
KR20060009884A (ko) 2006-02-01
IL171536A (en) 2013-02-28
WO2004096797A1 (en) 2004-11-11

Similar Documents

Publication Publication Date Title
ECSP056127A (es) Inhibidores de 3-quinasa de fosfatidil-inositol
ECSP066383A (es) Derivados de 5-fenil-4-metil-tiazol-2-il-amina como inhibidores de enzimas de cinasa fosfatidilinositol 3 (pi3) para el tratamiento de enfermedades inflamatorias de las vías respiratorias
NO2023022I1 (no) cobimetinib, optionally in any form protected by the basic patent, including harmaceutically acceptable salts and sovates thereof, particularly cobimetinib hemifumarate
ECSP105253A (es) Derivados de 5-feniltiazol y uso como inhibidores de pi3 cinasa
ECSP055582A (es) Derivados de benzotiazol que tienen actividad agonista de beta-2-adrenorreceptor
ATE433447T1 (de) Pyrimiidinverbindungen
CO6331340A2 (es) Pirrolo-pirimidinas y pirrolo piridinas
GB0305152D0 (en) Organic compounds
SE0202539D0 (sv) Compounds
CY1112960T1 (el) Παραγωγα ουριας, μεθοδοι για την παρασκευη τους και χρησεις αυτων
BRPI0409198A (pt) derivados quinolin-2-ona para o tratamento de doenças de vias aéreas
ECSP056134A (es) Derivados de quinuclidina que se enlazan con los receptores muscarínicos m3
ECSP066898A (es) Antagonistas de cgrp seleccionados, procedimiento para su preparación así como su uso como medicamento
GT200400133AA (es) Derivados de pirrolo[3,4-c] pirazol, activos como inhibidores de quinasa, proceso para su preparacion y composiciones farmaceuticas que los comprenden. (solicitud fraccionaria no. 1, derivada de la patente no. pi-2004-0133).
SV2004001690A (es) Nuevos derivados de fluoroglicosidos heterociclicos, medicamentos que contienen estos compuestos, y el uso de los mismos
CY1110034T1 (el) Παραγωγα 1,2,4,5-τετραϋδρο-3h-βενζαζεπινων, μεθοδος παρασκευης αυτων και οι φαρμακευτικες συνθεσεις που τα περιεχουν
UY28333A1 (es) Inhibidores de caspasa y sus usos.
SE0302192D0 (sv) Novel compounds
DE602004008959D1 (de) Benzoäbüä1,4üdioxepinderivate
CR9182A (es) Derivado de quinolina, su uso, preparacion y medicamento que lo contiene
PA8568101A1 (es) Indolil-urea derivados de tienopiridinas utiles como agentes antiangiogenicos, y procedimientos para su uso
SE0402925D0 (sv) Novel Compounds
SE0401763D0 (sv) Compounds
SE0403085D0 (sv) Novel componds
SE0403086D0 (sv) Compounds