PE20070978A1 - COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) - Google Patents

COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)

Info

Publication number
PE20070978A1
PE20070978A1 PE2007000145A PE2007000145A PE20070978A1 PE 20070978 A1 PE20070978 A1 PE 20070978A1 PE 2007000145 A PE2007000145 A PE 2007000145A PE 2007000145 A PE2007000145 A PE 2007000145A PE 20070978 A1 PE20070978 A1 PE 20070978A1
Authority
PE
Peru
Prior art keywords
pyridin
amino
pi3ks
phosphatidylinositol
kinases
Prior art date
Application number
PE2007000145A
Other languages
English (en)
Inventor
Zhi-Jie Ni
Sabina Pecchi
Matthew Burger
Wooseok Han
Aaron Smith
Gordana Atallah
Sarah Bartulis
Kelly Frazier
Joelle Verhagen
Yanchen Zhang
Ed Iwanowicz
Tom Hendrickson
Mark Knapp
Hanne Merritt
Charles Voliva
Marion Wiesmann
Darren Mark Legrand
Ian Bruce
James Dale
Jiong Lan
Barry Levine
Abran Costales
Jie Liu
Teresa Pick
Daniel Menezes
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 PE20070978A1 publication Critical patent/PE20070978A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

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

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE Q ES O U S; X ES CR3 O N; W ES C O N; V ES CR2, O U S; L1 ES CR9 O N, DONDE R2, R3, R7 Y R9 SON CADA UNO H, ALQUIL(C1-C10), ALQUENIL(C2-C6), ALCOXI(C1-C10), CICLOALQUIL(C3-C10), ENTRE OTROS; L2 ES CR6 O N, DONDE R4, R5 Y R6 SON CADA UNO H, HALOGENO, CN, NITRO, AMINO, ENTRE OTROS; R1 ES H, ALQUIL(C1-C10), ALCOXI(C1-C10), ARIL(C6-C14), CICLOALQUIL(C3-C10), ENTRE OTROS; R8 ES H, ALQUIL(C1-C10), CICLOALQUIL(C3-C7), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(6-(6-AMINO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)IMIDAZO[1.2-b]PIRIDAZIN-2-IL)ACETAMIDA, METIL 6-(6-AMINO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)IMIDAZO[1.2-a]PIRIDIN-2-ILCARBAMATO, N-(6-(6-AMINO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)-3-BROMO-IMIDAZO[1.2-a]PIRIDIN-2-IL)ACETAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) SIENDO UTILES EN EL TRATAMIENTO DE GLIOMA, MELANOMA, ASMA, FIBROSIS PULMONAR, PSORIASIS, DERMATITIS
PE2007000145A 2006-02-14 2007-02-12 COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) PE20070978A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US77347606P 2006-02-14 2006-02-14
US87672906P 2006-12-22 2006-12-22

Publications (1)

Publication Number Publication Date
PE20070978A1 true PE20070978A1 (es) 2007-11-15

Family

ID=38226373

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000145A PE20070978A1 (es) 2006-02-14 2007-02-12 COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)

Country Status (13)

Country Link
US (1) US20100075965A1 (es)
EP (1) EP1989201A1 (es)
JP (1) JP2009530233A (es)
KR (1) KR20080112202A (es)
AR (1) AR059506A1 (es)
AU (1) AU2007214462A1 (es)
BR (1) BRPI0707816A2 (es)
CA (1) CA2642738A1 (es)
MX (1) MX2008010397A (es)
PE (1) PE20070978A1 (es)
RU (1) RU2008136783A (es)
TW (1) TW200804379A (es)
WO (1) WO2007095588A1 (es)

Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007116432A1 (ja) 2006-03-30 2007-10-18 Aichi Prefecture キャノロールまたはそのプロドラッグ(pd)を含む抗炎症剤および癌予防剤ならびにこれらを含む医薬、化粧品および食品
US20100029619A1 (en) * 2006-08-04 2010-02-04 Takeda Pharmaceutical Company Limted Fused heterocyclic compound
AU2007291190A1 (en) 2006-08-30 2008-03-06 Cellzome Limited Triazole derivatives as kinase inhibitors
EP2099444A4 (en) 2006-12-14 2012-11-07 Nps Pharma Inc USE OF D-SERIN DERIVATIVES FOR THE TREATMENT OF ANTIBODIES
US8263585B2 (en) 2007-05-04 2012-09-11 Novartis Ag Organic compounds
US7928140B2 (en) 2007-08-02 2011-04-19 Amgen Inc. Benzothiazole PI3 kinase modulators for cancer treatment
EP2062893A1 (en) * 2007-10-18 2009-05-27 Bayer Schering Pharma AG Fused imidazoles for cancer treatment
MX2010001745A (es) * 2007-08-14 2010-03-10 Bayer Schering Pharma Ag Imidazoles fusionados para el tratamiento del cancer.
WO2009026254A1 (en) * 2007-08-17 2009-02-26 Icagen, Inc. Heterocycles as potassium channel modulators
US8431608B2 (en) 2007-08-17 2013-04-30 Icagen Inc. Heterocycles as potassium channel modulators
AU2008291075A1 (en) 2007-08-31 2009-03-05 Merck Serono S.A. Triazolopyridine compounds and their use as ask inhibitors
BRPI0819606A2 (pt) * 2007-11-27 2017-05-09 Cellzome Ltd amino triazóis como inobidores de pi3k
WO2009085230A1 (en) * 2007-12-19 2009-07-09 Amgen Inc. Inhibitors of pi3 kinase
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
US20090258907A1 (en) * 2008-04-09 2009-10-15 Abbott Laboratories Compounds useful as inhibitors of rock kinases
MX2010011370A (es) * 2008-04-16 2010-12-15 Vertex Pharma Inhibidores de fosfatidilinositol 3-cinasa.
JPWO2009128520A1 (ja) 2008-04-18 2011-08-04 塩野義製薬株式会社 Pi3k阻害活性を有する複素環化合物
WO2009133127A1 (en) * 2008-04-30 2009-11-05 Merck Serono S.A. Fused bicyclic compounds and use thereof as pi3k inhibitors
WO2009155052A1 (en) * 2008-05-28 2009-12-23 Wyeth 3-substituted-1h-pyrrolo[2,3-b]pyridine and 3-substituted-1h-pyrrolo[3,2-b]pyridine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2307400B1 (en) 2008-05-30 2014-04-23 Amgen, Inc Inhibitors of pi3 kinase
CN102131389A (zh) 2008-06-20 2011-07-20 健泰科生物技术公司 三唑并吡啶jak抑制剂化合物和方法
AU2009259867A1 (en) 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine JAK inhibitor compounds and methods
EP2311842A3 (en) * 2008-06-24 2011-07-13 Takeda Pharmaceutical Company Limited PI3K/M TOR inhibitors
WO2010007099A1 (en) * 2008-07-15 2010-01-21 Cellzome Limited 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors
WO2010007100A1 (en) * 2008-07-15 2010-01-21 Cellzome Ltd 7-substituted amino triazoles as pi3k inhibitors
WO2010057877A1 (en) * 2008-11-18 2010-05-27 Cellzome Limited 7-pyridinyl- or phenyl- substituted triazolo [1, 5 -a] pyridines as pi3k inhibitors
CN102300862B (zh) 2008-12-19 2016-11-23 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
WO2010092015A1 (en) 2009-02-10 2010-08-19 Cellzome Limited Urea triazololo [1, 5-a] pyridine derivatives as pi3k inhibitors
WO2010092041A1 (en) 2009-02-13 2010-08-19 Fovea Pharmaceuticals Sa [1, 2, 4] triazolo [1, 5 -a] pyridines as kinase inhibitors
JP2012518011A (ja) 2009-02-17 2012-08-09 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−キナーゼのテトラヒドロチアゾロピリジン阻害剤
WO2010135014A1 (en) * 2009-02-27 2010-11-25 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
WO2010100144A1 (en) * 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase
CA2755285C (en) 2009-03-20 2014-02-11 Yunxin Y. Bo Inhibitors of pi3 kinase
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
WO2010133534A1 (en) * 2009-05-19 2010-11-25 Cellzome Limited Bicyclic amino substituted compounds as pi3k inhibitors
WO2010133318A1 (en) * 2009-05-20 2010-11-25 Cellzome Ag Methods for the identification of phosphatidylinositol kinase interacting molecules and for the purification of phosphatidylinositol kinase proteins
WO2010141796A2 (en) 2009-06-05 2010-12-09 Cephalon, Inc. PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES
SI2448938T1 (sl) 2009-06-29 2014-08-29 Incyte Corporation Experimental Station Pirimidinoni kot zaviralci pi3k
EP2448946B1 (en) 2009-07-02 2013-07-24 Novartis AG 2-carboxamide cycloamino ureas useful as pi3k inhibitors
US8293753B2 (en) * 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
NZ598220A (en) * 2009-08-17 2014-02-28 Intellikine Llc Heterocyclic compounds and uses thereof
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
US9193721B2 (en) 2010-04-14 2015-11-24 Incyte Holdings Corporation Fused derivatives as PI3Kδ inhibitors
US8487102B2 (en) * 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
WO2011137155A1 (en) 2010-04-28 2011-11-03 Bristol-Myers Squibb Company Imidazopyridazinyl compounds and their uses for cancer
EP2569286B1 (en) * 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
NZ603477A (en) 2010-05-12 2014-09-26 Vertex Pharma Compounds useful as inhibitors of atr kinase
JP5856151B2 (ja) * 2010-05-12 2016-02-09 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Vertex Pharmaceuticals Incorporated Atrキナーゼ阻害剤として有用な2−アミノピリジン誘導体
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
CN103153062B (zh) * 2010-05-24 2015-07-15 因特利凯有限责任公司 杂环化合物及其用途
TW201204723A (en) 2010-06-22 2012-02-01 Fovea Pharmaceuticals Heterocyclic compounds, their preparation and their therapeutic application
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン
EP2665704A1 (en) * 2011-01-19 2013-11-27 Galapagos NV Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン, エルエルシー 複素環化合物およびその使用
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
EP2694510B1 (en) 2011-04-07 2015-10-14 Bayer Intellectual Property GmbH Imidazopyridazines as akt kinase inhibitors
CA2846652C (en) 2011-09-02 2019-11-05 Incyte Corporation Heterocyclylamines as pi3k inhibitors
EP2940017B1 (en) 2011-09-30 2019-08-28 Vertex Pharmaceuticals Incorporated Process for making compounds useful as inhibitors of ATR kinase
MX2014003785A (es) 2011-09-30 2014-07-24 Vertex Phamaceuticals Inc Tratamiento del cancer de pancreas y del cancer de pulmon de celulas no pequeñas con inhibidores de atr.
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
NZ720511A (en) 2012-04-05 2016-12-23 Vertex Pharma Compounds useful as inhibitors of atr kinase and combination therapies thereof
MX2014013725A (es) 2012-05-23 2015-02-10 Hoffmann La Roche Composiciones y metodos para obtener y utilizar celulas del endodermo y hepatocitos.
CN104619709B (zh) * 2012-07-13 2016-11-09 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
WO2014144850A1 (en) 2013-03-15 2014-09-18 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
TW201514143A (zh) * 2013-03-20 2015-04-16 Hoffmann La Roche 新穎脲衍生物
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
MX2016006815A (es) 2013-11-27 2016-12-02 Signalchem Lifesciences Corp Derivados de aminopiridina como inhibidores de cinasas de la familia de tyro3, axl y mer (tam).
GB201321733D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
TWI720451B (zh) 2014-02-13 2021-03-01 美商英塞特控股公司 作為lsd1抑制劑之環丙胺
US9670210B2 (en) 2014-02-13 2017-06-06 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
WO2015134171A1 (en) 2014-03-06 2015-09-11 Takeda Pharmaceutical Company Limited Heteroarylamide inhibitors of tbk1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
ES2760507T3 (es) * 2014-12-19 2020-05-14 Janssen Pharmaceutica Nv Derivados de imidazopiridazina enlazados a heterociclilo como inhibidores de PI3Kß
ES2843522T3 (es) 2015-02-27 2021-07-19 Incyte Corp Sales del inhibidor de PI3K y procesos para su preparación
EA201792205A1 (ru) 2015-04-03 2018-02-28 Инсайт Корпорейшн Гетероциклические соединения как ингибиторы lsd1
CN107849022A (zh) 2015-04-10 2018-03-27 亚瑞克西斯制药公司 取代的喹唑啉化合物和其使用方法
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
AU2016306555B2 (en) 2015-08-12 2021-01-28 Incyte Holdings Corporation Salts of an LSD1 inhibitor
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017059357A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
US10414757B2 (en) 2015-11-16 2019-09-17 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017152126A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
US10166221B2 (en) 2016-04-22 2019-01-01 Incyte Corporation Formulations of an LSD1 inhibitor
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
CN110036010A (zh) 2016-09-29 2019-07-19 亚瑞克西斯制药公司 Kras g12c突变蛋白的抑制剂
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
EP3630747A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Quinazoline derivatives as modulators of mutant kras, hras or nras
US10669246B2 (en) * 2017-10-02 2020-06-02 1ST Biotherapeutics, Inc. Benzothiazol compounds and methods using the same for treating neurodegenerative disorders
HRP20220297T1 (hr) * 2017-10-30 2022-05-13 Bristol-Myers Squibb Company Aminoimidazopiridazini kao inhibitori kinaze
IL275490B2 (en) * 2017-12-22 2024-05-01 Ravenna Pharmaceuticals Inc Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
MX2020006613A (es) * 2017-12-22 2020-11-13 Ravenna Pharmaceuticals Inc Derivados de aril-bipiridina amina como inhibidores de fosfatidilinositol fosfato cinasa.
EP3749305A1 (en) * 2018-02-05 2020-12-16 Université de Strasbourg Compounds and compositions for the treatment of pain
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
AU2020224401A1 (en) * 2019-02-22 2021-10-14 1ST Biotherapeutics, Inc. Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders
US20220160902A1 (en) * 2019-03-07 2022-05-26 1ST Biotherapeutics, Inc. [18F]-Labeled Benzothiazole Derivative As PET Radiotracer
US10385046B1 (en) 2019-03-19 2019-08-20 1ST Biotherapeutics, Inc. Processes for preparing benzothiazol compounds and methods of using the same for treating neurodegenerative disorders
JP2022527169A (ja) * 2019-03-28 2022-05-31 ファースト・バイオセラピューティクス・インコーポレイテッド ベンゾチアゾール化合物の薬学的塩、多形体及びその製造方法
WO2020201773A1 (en) * 2019-04-05 2020-10-08 Storm Therapeutics Ltd Mettl3 inhibitory compounds
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
CN112047950B (zh) * 2020-09-14 2023-07-25 华东师范大学 咪唑并吡嗪类衍生物及其合成方法和应用
JP2023541464A (ja) * 2020-09-15 2023-10-02 ファースト・バイオセラピューティクス・インコーポレイテッド 2-アミノ-3-カルボニルイミダゾピリジン及びピラゾロピリジン化合物
US11834467B2 (en) 2020-09-28 2023-12-05 1ST Biotherapeutics, Inc. Substituted indazoles as hematopoietic progenitor kinase 1 (HPK1) inhibitors
WO2023134692A1 (zh) * 2022-01-13 2023-07-20 浙江同源康医药股份有限公司 多环类化合物及其用途

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6041077B2 (ja) * 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4323581A (en) * 1978-07-31 1982-04-06 Johnson & Johnson Method of treating carcinogenesis
IL73534A (en) * 1983-11-18 1990-12-23 Riker Laboratories Inc 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds
US4904768A (en) * 1987-08-04 1990-02-27 Bristol-Myers Company Epipodophyllotoxin glucoside 4'-phosphate derivatives
US5238944A (en) * 1988-12-15 1993-08-24 Riker Laboratories, Inc. Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
US4929624A (en) * 1989-03-23 1990-05-29 Minnesota Mining And Manufacturing Company Olefinic 1H-imidazo(4,5-c)quinolin-4-amines
US5389640A (en) * 1991-03-01 1995-02-14 Minnesota Mining And Manufacturing Company 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines
US5451700A (en) * 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
US5268376A (en) * 1991-09-04 1993-12-07 Minnesota Mining And Manufacturing Company 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines
GB9300059D0 (en) * 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
US5621100A (en) * 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5395937A (en) * 1993-01-29 1995-03-07 Minnesota Mining And Manufacturing Company Process for preparing quinoline amines
US5352784A (en) * 1993-07-15 1994-10-04 Minnesota Mining And Manufacturing Company Fused cycloalkylimidazopyridines
EP0708772B1 (en) * 1993-07-15 2000-08-23 Minnesota Mining And Manufacturing Company IMIDAZO [4,5-c]PYRIDIN-4-AMINES
IT1261907B (it) * 1993-09-15 1996-06-03 Sasib Spa Dispositivo alimentatore di foglietti con ruota di confezionamento, in particolare nelle macchine impacchettatrici di sigarette.
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5482936A (en) * 1995-01-12 1996-01-09 Minnesota Mining And Manufacturing Company Imidazo[4,5-C]quinoline amines
GB9508538D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US6331555B1 (en) * 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) * 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
KR100447918B1 (ko) * 1996-07-25 2005-09-28 동아제약주식회사 대장을포함한위장관보호작용을갖는플라본및플라바논화합물
CO4950519A1 (es) * 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6166037A (en) * 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
MXPA02007632A (es) * 2000-02-07 2004-08-23 Abbott Gmbh & Co Kg Derivados de 2-benzotiazolil urea y su uso como inhibidores de proteina cinasa.
EP1317442B1 (en) * 2000-09-11 2005-11-16 Chiron Corporation Quinolinone derivatives as tyrosine kinase inhibitors
HUP0303494A3 (en) * 2000-12-15 2009-08-28 Vertex Pharma Parmaceutical compositions containing bacterial gyrase inhibitors and uses thereof
US20030134846A1 (en) * 2001-10-09 2003-07-17 Schering Corporation Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors
WO2003077902A1 (en) * 2002-02-19 2003-09-25 Xenoport, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
US6900342B2 (en) * 2002-05-10 2005-05-31 Dabur India Limited Anticancer taxanes such as paclitaxel, docetaxel and their structural analogs, and a method for the preparation thereof
DK1603570T5 (da) * 2003-02-26 2013-12-09 Sugen Inc Aminoheteroarylforbindelser som proteinkinaseinhibitorer
WO2005035526A1 (en) * 2003-10-09 2005-04-21 Argenta Discovery Ltd. Bicyclic compounds and their therapeutic use
ATE438400T1 (de) * 2004-03-19 2009-08-15 Warner Lambert Co Imidazopyridin- und imidazopyrimidin-derivate als antibakterielle mittel
US20100029619A1 (en) * 2006-08-04 2010-02-04 Takeda Pharmaceutical Company Limted Fused heterocyclic compound

Also Published As

Publication number Publication date
EP1989201A1 (en) 2008-11-12
AU2007214462A1 (en) 2007-08-23
BRPI0707816A2 (pt) 2011-05-10
WO2007095588A1 (en) 2007-08-23
CA2642738A1 (en) 2007-08-23
TW200804379A (en) 2008-01-16
RU2008136783A (ru) 2010-03-20
AR059506A1 (es) 2008-04-09
KR20080112202A (ko) 2008-12-24
US20100075965A1 (en) 2010-03-25
MX2008010397A (es) 2008-10-27
JP2009530233A (ja) 2009-08-27

Similar Documents

Publication Publication Date Title
PE20070978A1 (es) COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
PE20081887A1 (es) Nuevo compuesto de adenina
PE20121482A1 (es) Derivados de imidazopiridina como inhibidores de jak
PE20121352A1 (es) Derivados de heteroarilo que contienen n como inhibidores de cinasa jak3
ES2721018T3 (es) N-Acil-(3-sustituido)-(8-metil)-5,6-dihidro-[1,2,4]triazolo[4,3-a]pirazinas como antagonistas selectivos del receptor NK-3, composición farmacéutica, métodos para su uso en trastornos mediados por el receptor de NK-3
PE20091734A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
CL2008001818A1 (es) Ácido {4,6-bis(dimetilamino)-2-(4-(4-(trifluorometil)benzamido)bencil)pirimidin-5-il}acético amorfo y sus formas cristalinas i y ii; proceso de preparación; composición farmacéutica; y uso en el tratamiento de enfermedades inflamatorias tales como asma, rinitis alérgica, crohn, entre otras.
PE20130779A1 (es) Pirimidinas y triazinas condensadas y su uso
PE20151249A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
PE20120418A1 (es) DERIVADOS DE PIRIDO[2,3-b]PIRAZINA COMO INHIBIDORES DE POLI (ADP-RIBOSA) POLIMERASA (PARP)
PE20110584A1 (es) DERIVADOS DE IMIDAZO[1,2-a]PIRIMIDINA COMO INHIBIDORES DE MET, COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN Y SU PROCEDIMIENTO DE PREPARACION
PE20110411A1 (es) Imidazopiridazinacarbonitrilos como inhibidores de quinasa
PE20110398A1 (es) BENZAMIDAS CON ACTIVIDAD SOBRE LA ENZIMA p38 MAP-QUINASA
BRPI0507065A (pt) derivados de quinolina e seu uso como inibidores micobacterianos
PE20090773A1 (es) Derivados de morfolina pirimidina
MX2010004819A (es) Derivados de [1h-pirazolo[3,4-b]piridin-4-il]-fenilo o piridin-2-ilo como proteina cinasa c-theta.
PT1513826E (pt) Novos derivados de indolilpiperidina como agentes anti-histaminicos e antialergicos potentes
PE20170666A1 (es) 2-(morfolin-4-il)-1,7-naftiridinas
ECSP066504A (es) Derivados biciclicos [3.1.0] como inhibidores del transportador de glicina
PE20170003A1 (es) Compuestos heterociclicos y usos de los mismos
CL2008001274A1 (es) Compuestos macrolidos derivados de 5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahidrociclopropan[e]pirrolo[1,2-a][1,4]diazaciclopentadecinilo, inhibidores de la actividad de la proteasa ns3-ns4; su procedimiento de preparacion; composicion farmaceutica; compuestos intermediarios y procedimiento de preparacion; y uso en el tratamiento de.....
PE20061098A1 (es) COMPUESTOS IMIDAZO[1,2-a] PIRIDINILO COMO INHIBIDORES DE VEGF-R2
PE20110560A1 (es) NUEVOS DERIVADOS DE TRIAZOLO[4,3-a]PIRIDINA, SU PROCEDIMIENTO DE PREPARACION, SU APLICACION COMO MEDICAMENTOS, COMPOSICIONES FARMACEUTICAS Y NUEVA UTILIZACION PARTICULARMENTE COMO INHIBIDORES DE MET
CL2012001329A1 (es) Procedimiento de purificacion de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo-[3,4-b]piridin-3-il] pirimidin-5-il} metilcarbamato de metilo; y el compuesto intermediario que se obtiene.
PE20061297A1 (es) Compuestos derivados de cromano y cromeno moduladores del receptor de serotonina 5-ht2c

Legal Events

Date Code Title Description
FD Application declared void or lapsed