ATE445614T1 - Phosphatidylinositol 3-kinase inhibitoren - Google Patents

Phosphatidylinositol 3-kinase inhibitoren

Info

Publication number
ATE445614T1
ATE445614T1 AT04730527T AT04730527T ATE445614T1 AT E445614 T1 ATE445614 T1 AT E445614T1 AT 04730527 T AT04730527 T AT 04730527T AT 04730527 T AT04730527 T AT 04730527T AT E445614 T1 ATE445614 T1 AT E445614T1
Authority
AT
Austria
Prior art keywords
phosphatidylinositol
kinase inhibitors
kinase
inhibitors
Prior art date
Application number
AT04730527T
Other languages
English (en)
Inventor
Ian Bruce
Bernard Cuenoud
Thomas Keller
Gaynor Pilgrim
Nicola Press
Grand Darren Le
Cathy Ritchie
Barbara Valade
Judy Hayler
Emma Budd
Original Assignee
Novartis Pharma Gmbh
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 Pharma Gmbh filed Critical Novartis Pharma Gmbh
Application granted granted Critical
Publication of ATE445614T1 publication Critical patent/ATE445614T1/de

Links

Classifications

    • 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
    • A61K31/535Heterocyclic 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
    • 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
    • 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
    • C07D417/14Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT04730527T 2003-05-02 2004-04-30 Phosphatidylinositol 3-kinase inhibitoren ATE445614T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0310234 2003-05-02
PCT/EP2004/004603 WO2004096797A1 (en) 2003-05-02 2004-04-30 Inhibitors of phosphatidylinositol 3-kinase

Publications (1)

Publication Number Publication Date
ATE445614T1 true ATE445614T1 (de) 2009-10-15

Family

ID=33397059

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04730527T ATE445614T1 (de) 2003-05-02 2004-04-30 Phosphatidylinositol 3-kinase inhibitoren

Country Status (28)

Country Link
US (3) US20070032487A1 (de)
EP (2) EP2157091B1 (de)
JP (1) JP4510807B2 (de)
KR (1) KR100725885B1 (de)
CN (2) CN1816549B (de)
AR (1) AR044519A1 (de)
AT (1) ATE445614T1 (de)
AU (2) AU2004234068B2 (de)
BR (1) BRPI0410037B8 (de)
CA (1) CA2524401C (de)
CL (1) CL2004000917A1 (de)
DE (1) DE602004023602D1 (de)
EC (1) ECSP056127A (de)
ES (2) ES2546851T3 (de)
HK (1) HK1091810A1 (de)
IL (1) IL171536A (de)
IS (1) IS8152A (de)
MA (1) MA27774A1 (de)
MX (1) MXPA05011740A (de)
NO (1) NO20055714L (de)
PE (1) PE20050147A1 (de)
PL (1) PL1622897T3 (de)
PT (1) PT1622897E (de)
RU (2) RU2384580C2 (de)
TN (1) TNSN05278A1 (de)
TW (1) TW200519106A (de)
WO (1) WO2004096797A1 (de)
ZA (1) ZA200508603B (de)

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
WO2006066172A1 (en) * 2004-12-17 2006-06-22 Amgen, Inc. Aminopyrimidine compounds and methods of use
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
WO2006125805A1 (en) * 2005-05-24 2006-11-30 Laboratoires Serono S.A. Thiazole derivatives and use thereof
EA017166B1 (ru) 2005-05-24 2012-10-30 Мерк Сероно С.А. Производные тиазола и их применение
WO2006135604A2 (en) * 2005-06-09 2006-12-21 Merck & Co., Inc. 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
EA200801716A1 (ru) * 2006-01-18 2009-04-28 Амген Инк. Тиазольные соединения и их применение
EP1991528A2 (de) * 2006-01-18 2008-11-19 Siena Biotech S.p.A. Modulatoren von alpha7-nicotinischen acetylcholinrezeptoren und therapeutische verwendungen davon
CA2635830A1 (en) * 2006-01-23 2007-07-26 Laboratoires Serono S.A. Thiazole derivatives and use thereof
US8217037B2 (en) * 2006-04-07 2012-07-10 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
EP2016075A1 (de) * 2006-05-03 2009-01-21 AstraZeneca AB Thiazolderivate und ihre verwendung als antitumormittel
GB0612630D0 (en) 2006-06-26 2006-08-02 Novartis Ag Organic compounds
EP2061787A2 (de) * 2006-09-01 2009-05-27 Vertex Pharmaceuticals Incorporated 5-(2-furyl)-1,3-thiazol-derivate als hemmer von phosphatidylinositol-3-kinase
GB0620059D0 (en) * 2006-10-10 2006-11-22 Ucb Sa Therapeutic agents
GB0620818D0 (en) * 2006-10-19 2006-11-29 Ucb Sa Therapeutic agents
EP2129379B1 (de) * 2007-02-20 2019-04-10 Novartis AG Imidazochinoline als doppellipidkinase- und mtor-hemmer
TW200906825A (en) * 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
EP2166843A4 (de) 2007-06-01 2010-08-11 Univ Princeton Behandlung von virusinfektionen durch modulation von hostzellen-stoffwechselpfaden
EP2173728A2 (de) 2007-07-17 2010-04-14 Amgen Inc. Heterocyclische pkb-modulatoren
AU2008276512A1 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of PKB
EP2238134A2 (de) * 2007-12-20 2010-10-13 Novartis AG Bis-Thiazol-Derivate, ihr Herstellungsverfahren und ihre Verwendung als Arzneimittel
KR20100093129A (ko) * 2007-12-20 2010-08-24 노파르티스 아게 Pi 3 키나제 억제제로서 사용되는 티아졸 유도체
WO2009094224A1 (en) 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
CA2716898A1 (en) 2008-02-27 2009-09-03 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
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
CA2750935A1 (en) * 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
JPWO2010125799A1 (ja) * 2009-04-27 2012-10-25 塩野義製薬株式会社 Pi3k阻害活性を有するウレア誘導体
ME02900B (de) * 2009-04-30 2018-04-20 Glaxo Group Ltd Neuartige verbindungen
EP2440556A1 (de) * 2009-06-10 2012-04-18 Vertex Pharmaceuticals Incorporated Phosphatidylinositol 3-kinasehemmer
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
UY32748A (es) 2009-07-02 2011-01-31 Novartis Ag 2-carboxamida-cicloamino-ureas
WO2011048936A1 (ja) 2009-10-19 2011-04-28 大正製薬株式会社 アミノチアゾール誘導体
BR112012019459A2 (pt) 2010-02-03 2017-10-17 Signal Pharm Llc identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase.
MX2013001660A (es) 2010-08-11 2013-06-03 Millenium Pharmaceuticals Inc Heteroarilos y usos de los mismos.
WO2012021615A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012051410A2 (en) 2010-10-13 2012-04-19 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US20130209461A1 (en) * 2010-11-08 2013-08-15 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
PE20140601A1 (es) * 2011-04-25 2014-05-24 Novartis Ag COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K) Y UN INHIBIDOR DE mTOR
MX359406B (es) 2011-07-01 2018-09-27 Novartis Ag Terapia de combinación que comprende un inhibidor de cdk4/6 y un inhibidor de pi3kpara usarse en el tratamiento de cáncer.
US20130158023A1 (en) 2011-08-03 2013-06-20 Signal Pharmaceuticals, Llc Identification of gene expression 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
WO2013148912A1 (en) * 2012-03-30 2013-10-03 Novartis Ag Compounds for use in the treatment of neuroblastoma, ewing's sarcoma or rhabdomyosarcoma
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 (de) 2012-12-13 2017-12-06 IP Gesellschaft für Management mbH Kombinationstherapie mit einem cdk4/6-hemmer und einem pi3k-hemmer zur verwendung bei der behandlung von krebs
TWI628170B (zh) 2013-02-05 2018-07-01 先正達合夥公司 植物生長調節化合物
BR112015026292B1 (pt) 2013-04-17 2022-04-12 Signal Pharmaceuticals, Llc Uso de 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino [2,3-b]pirazin-2(1h)- ona e métodos in vitro
KR20160002792A (ko) 2013-04-17 2016-01-08 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 n-(3-(5-플루오로-2-(4-(2-메톡시에톡시)페닐아미노)피리미딘-4-일아미노)페닐)아크릴아미드를 포함하는 병용 요법
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
UA115805C2 (uk) 2013-04-17 2017-12-26 Сігнал Фармасьютікалз, Елелсі Комбінована терапія, яка включає сполуку дигідропіразинопіразину й антагоніст рецептора андрогену, для лікування раку простати
AU2014254050B2 (en) 2013-04-17 2018-10-04 Signal Pharmaceuticals, Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 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
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
KR102271344B1 (ko) 2013-04-17 2021-07-01 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
CN105407892B (zh) 2013-05-29 2019-05-07 西格诺药品有限公司 一种化合物的药物组合物、其固体形式及它们的使用方法
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
EP3131551A4 (de) 2014-04-16 2017-09-20 Signal Pharmaceuticals, LLC Feste formen mit 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)-on und co-former, zusammensetzungen und verfahren zu deren verwendung
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
US11091472B2 (en) 2016-02-26 2021-08-17 The Regents Of The University Of California PI-kinase inhibitors with anti-infective activity
JP7282045B2 (ja) 2017-06-22 2023-05-26 セルジーン コーポレイション B型肝炎ウイルス感染を特徴とする肝細胞癌の治療
US11325900B2 (en) 2018-01-15 2022-05-10 Aucentra Holdings Pty Ltd 5-(pyrimidin-4-yl)thiazol-2-yl urea derivatives as therapeutic agents
JP7309725B2 (ja) 2018-08-21 2023-07-18 杏林製薬株式会社 2環性ヘテロ芳香環誘導体
AU2021206651B2 (en) * 2020-01-07 2024-02-22 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
EP0373226B1 (de) 1988-04-15 1994-06-15 Taiho Pharmaceutical Company, Limited Carbamoyl-2-Pyrrolidinonverbindungen
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
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
EP0946587A2 (de) 1996-12-16 1999-10-06 Fujisawa Pharmaceutical Co., Ltd. Amindverbindungen und ihre verwendung als inhibitoren der bitric-oxid-synthase
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
EP1027050B1 (de) 1997-10-27 2004-01-14 Takeda Chemical Industries, Ltd. 1,3-thiazole als adenosine a3 rezeptor antagonisten zur behandlung von asthma, allergien und diabetes
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
GB9723589D0 (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
DE69923681T2 (de) 1998-06-18 2006-01-12 Bristol-Myers Squibb Co. Kohlenstoff substituierte aminothiazole als inhibitoren von cyclin-abhängigen kinasen
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
ATE246701T1 (de) 1998-06-23 2003-08-15 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivate
GB9813535D0 (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
EP1098923B1 (de) 1998-06-30 2004-11-17 Dow Global Technologies Inc. Polymerpolyole und ein verfahren zu ihrer darstellung
DE69932173T2 (de) 1998-10-16 2007-06-06 Pfizer Inc. Adeninderivate
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
SK286666B6 (sk) * 1999-04-23 2009-03-05 Takeda Pharmaceutical Company Limited 5-Pyridyl-1,3-azolové zlúčeniny, spôsob výroby a použitia
EP1659111A3 (de) 1999-05-04 2007-05-09 Schering Corporation Piperidinderivate verwendbar als ccr5 antagonisten
BR0010304A (pt) 1999-05-04 2002-02-13 Schering Corp Derivados de piperazina úteis como antagonistas do ccr5
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.
CZ2002861A3 (cs) * 1999-09-10 2002-06-12 Merck & Co., Inc. Inhibitory tyrosinkinázy
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
WO2001072745A1 (en) 2000-03-29 2001-10-04 Cyclacel Limited 2-substituted 4-heteroaryl-pyrimidines and their use in the treatmetn of proliferative disorders
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
PL201530B1 (pl) 2000-06-27 2009-04-30 L V A T Lab Sa Karbaminiany pochodne aryloalkiloamin i zastosowanie karbaminianów pochodnych aryloalkiloamin
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
AU2001275760B2 (en) 2000-08-05 2005-03-17 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
KR100589032B1 (ko) 2000-10-20 2006-06-14 에자이 가부시키가이샤 질소 함유 방향환 유도체
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
IL156499A0 (en) 2000-12-22 2004-01-04 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as m3 antagonists
JP4295985B2 (ja) 2000-12-28 2009-07-15 ラボラトリオス・アルミラル・ソシエダッド・アノニマ 新規なキヌクリジン誘導体およびそれを含む医薬組成物
EP1241176A1 (de) 2001-03-16 2002-09-18 Pfizer Products Inc. Purinderivate zur Behandlung von Ischämie
ES2314052T3 (es) 2001-04-30 2009-03-16 Glaxo Group Limited Derivados de ester de 17beta-carbotioato de androstano con un grupo ester ciclico en la posicion 17alfa.
ATE315555T1 (de) 2001-05-11 2006-02-15 Pfizer Prod Inc Thiazolderivate und ihre verwendung als cdk- inhibitoren
SK14302003A3 (sk) 2001-05-25 2004-08-03 Kombinácia agonistu adenozín A2a receptora a anticholinergického činidla na ošetrovanie obštrukčných chorôb dýchacích ciest
US20040248867A1 (en) 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
EP2039762A3 (de) 2001-06-21 2009-07-29 Verenium Corporation Nitralasen
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
WO2003015778A1 (en) 2001-08-17 2003-02-27 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1430051B1 (de) 2001-09-28 2006-12-27 Cyclacel Limited N-(4-(4-methylthiazol-5-yl)pyrimidin-2-yl)-n-phenylamine als antiproliferative verbindungen
CA2462980A1 (en) 2001-10-17 2003-04-24 Ucb, S.A. Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
MY130622A (en) 2001-11-05 2007-07-31 Novartis Ag Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors
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
MXPA04006206A (es) 2001-12-20 2004-12-06 S A L V A T Lab Sa Derivados de 1-alquil-azoniabiciclo(2.2.2(octano carbamato y su uso como antagonistas del receptor musrcarinico.
WO2003072592A1 (en) 2002-01-15 2003-09-04 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
AU2003230700A1 (en) 2002-03-26 2003-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2003218342B8 (en) 2002-03-26 2008-07-31 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1496911B1 (de) 2002-04-10 2007-12-19 University Of Virginia Patent Foundation Verwendung von a2a adenosin rezeptor agonisten und anti-pathogene mittel enthaltenden kombinationen zur behandlung von entzündungskrankheiten
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
ES2282667T3 (es) 2002-06-25 2007-10-16 Merck Frosst Canada Ltd. Inhibidores de pde4 8-(biaril)quinolinas.
JP2005538972A (ja) 2002-07-02 2005-12-22 メルク フロスト カナダ アンド カンパニー ジアリール置換エタンピリドンpde4阻害剤
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
DK1521733T3 (da) 2002-07-08 2014-10-13 Pfizer Prod Inc Modulatorer af glucocorticoid receptoren
PE20050130A1 (es) 2002-08-09 2005-03-29 Novartis Ag Compuestos organicos
JP2006514684A (ja) 2002-10-30 2006-05-11 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 Rockおよび他のプロテインキナーゼとして有用な組成物
WO2004045518A2 (en) 2002-11-15 2004-06-03 Bristol-Myers Squibb Company Open chain prolyl urea-related 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
ZA200602755B (en) 2003-09-06 2007-06-27 Vertex Pharma Modulators of ATP-binding cassette transporters
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
EA017166B1 (ru) 2005-05-24 2012-10-30 Мерк Сероно С.А. Производные тиазола и их применение
WO2006125805A1 (en) 2005-05-24 2006-11-30 Laboratoires Serono S.A. Thiazole derivatives and use thereof
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
JP2009519346A (ja) 2005-12-12 2009-05-14 ジェネラブズ テクノロジーズ インコーポレーティッド N−(5員芳香族環)−アミド抗ウイルス化合物
GB0525671D0 (en) 2005-12-16 2006-01-25 Novartis Ag Organic compounds
CA2635830A1 (en) 2006-01-23 2007-07-26 Laboratoires Serono S.A. Thiazole derivatives and use thereof
GB0610243D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
JP2010510246A (ja) 2006-11-21 2010-04-02 スミスクライン ビーチャム コーポレーション アミド抗ウイルス化合物
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
AU2008257559B2 (en) 2007-05-25 2013-10-10 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (MGLU2 receptor)
US20090004140A1 (en) 2007-06-26 2009-01-01 Yao-Ling Qiu 4-substituted pyrrolidine as anti-infectives
US20100292236A1 (en) 2007-07-19 2010-11-18 H. Lundbeck A/S 5-Membered Heterocyclic Amides And Related Compounds
EP2238134A2 (de) * 2007-12-20 2010-10-13 Novartis AG Bis-Thiazol-Derivate, ihr Herstellungsverfahren und ihre Verwendung als Arzneimittel
KR20100093129A (ko) * 2007-12-20 2010-08-24 노파르티스 아게 Pi 3 키나제 억제제로서 사용되는 티아졸 유도체
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
US20130172349A1 (en) 2013-07-04
ECSP056127A (es) 2006-03-01
US20070032487A1 (en) 2007-02-08
EP1622897A1 (de) 2006-02-08
RU2384580C2 (ru) 2010-03-20
MA27774A1 (fr) 2006-02-01
EP2157091A1 (de) 2010-02-24
US8404684B2 (en) 2013-03-26
ZA200508603B (en) 2006-12-27
IL171536A (en) 2013-02-28
JP4510807B2 (ja) 2010-07-28
PT1622897E (pt) 2009-12-10
RU2005137358A (ru) 2006-07-27
CN101648949A (zh) 2010-02-17
JP2006525266A (ja) 2006-11-09
CN1816549B (zh) 2010-09-29
AU2008255157A1 (en) 2009-01-08
MXPA05011740A (es) 2006-01-26
TNSN05278A1 (en) 2007-07-10
RU2481346C2 (ru) 2013-05-10
BRPI0410037B8 (pt) 2021-05-25
EP2157091B1 (de) 2015-06-10
CA2524401C (en) 2011-11-22
HK1091810A1 (en) 2007-01-26
DE602004023602D1 (en) 2009-11-26
EP1622897B1 (de) 2009-10-14
US20110105535A1 (en) 2011-05-05
ES2546851T3 (es) 2015-09-29
TW200519106A (en) 2005-06-16
PE20050147A1 (es) 2005-05-05
NO20055714L (no) 2006-02-02
AU2004234068B2 (en) 2008-09-11
CN1816549A (zh) 2006-08-09
BRPI0410037A (pt) 2006-04-25
PL1622897T3 (pl) 2010-03-31
CA2524401A1 (en) 2004-11-11
AU2004234068A1 (en) 2004-11-11
ES2331883T3 (es) 2010-01-19
BRPI0410037B1 (pt) 2018-01-16
WO2004096797A1 (en) 2004-11-11
AR044519A1 (es) 2005-09-14
RU2009134044A (ru) 2011-03-20
KR100725885B1 (ko) 2007-06-08
KR20060009884A (ko) 2006-02-01
AU2008255157B2 (en) 2011-02-03
NO20055714D0 (no) 2005-12-02
IS8152A (is) 2005-11-25
CL2004000917A1 (es) 2005-02-11

Similar Documents

Publication Publication Date Title
ATE445614T1 (de) Phosphatidylinositol 3-kinase inhibitoren
DE602004018837D1 (de) Ptidase-iv-inhibitoren
ATE505471T1 (de) Azaindol-kinaseinhibitoren
ATE452891T1 (de) Pyrimidopyrimidone als kinaseinhibitoren
NO20055742D0 (no) Gjenget forbindelse for stalror
DE602004023168D1 (de) Plattenspeichersteuerwerk
NO20054852D0 (no) GFAT inhibitorer
DE60320933D1 (de) Rho-kinase inhibitoren
ATE404564T1 (de) Diazepinoindolderivate als kinaseinhibitoren
IS8352A (is) Ný rópínírólsamsetning
DK1692242T3 (da) Viskoelastisk syre
DE602004017623D1 (de) N-substituierte pyrazolyl-amidyl-benzimidazolyl-c-kit-inhibitoren
DE50308380D1 (de) Chirurgischer nagel
ATE433449T1 (de) Kinaseinhibitoren
ATE545642T1 (de) Mmp-inhibitoren
DE602004004230D1 (de) Klasse-D Verstärker
DE50308254D1 (de) Messgerät
DE602004013236D1 (de) Messgerät
IS7963A (is) Efnasambönd með hamlandi virkni gegn prólýlólígópeptíðasa
DE602004008130D1 (de) Messuhr
DE602004019720D1 (de) Platteneinheit
DE60328233D1 (de) Sulfamatbenzothiophenderivate als steroidsulfataseinhibitoren
DE502004004257D1 (de) Adapter f r autoradios
ATA12882003A (de) Osteosynthesevorrichtung
DE50309663D1 (de) Messtisch

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 1622897

Country of ref document: EP